Target Information

Target General Information

Top

Target ID

T60693 (Former ID: TTDS00127)

Target Name

Opioid receptor kappa (OPRK1)

Synonyms

OPRK; Kappa-type opioid receptor; Kappa opioid receptor; KOR-1; KOR; K-OR-1

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Gene Name

OPRK1

Target Type

Successful target

[1]

Disease

[+] 3 Target-related Diseases

Non-specific cutaneous vascular sympton [ICD-11: ME64]

Pain [ICD-11: MG30-MG3Z]

Pruritus [ICD-11: EC90]

Function

Functions as receptor for various synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling leads to the inhibition of adenylate cyclase activity. Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Plays a role in the perception of pain. Plays a role in mediating reduced physical activity upon treatment with synthetic opioids. Plays a role in the regulation of salivation in response to synthetic opioids. May play a role in arousal and regulation of autonomic and neuroendocrine functions. G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins.

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BioChemical Class

GPCR rhodopsin

UniProt ID

OPRK_HUMAN

Sequence

MDSPIQIFRGEPGPTCAPSACLPPNSSAWFPGWAEPDSNGSAGSEDAQLEPAHISPAIPV
IITAVYSVVFVVGLVGNSLVMFVIIRYTKMKTATNIYIFNLALADALVTTTMPFQSTVYL
MNSWPFGDVLCKIVISIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPLKAKIINI
CIWLLSSSVGISAIVLGGTKVREDVDVIECSLQFPDDDYSWWDLFMKICVFIFAFVIPVL
IIIVCYTLMILRLKSVRLLSGSREKDRNLRRITRLVLVVVAVFVVCWTPIHIFILVEALG
STSHSTAALSSYYFCIALGYTNSSLNPILYAFLDENFKRCFRDFCFPLKMRMERQSTSRV
RNTVQDPAYLRDIDGMNKPV

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3D Structure

Click to Show 3D Structure of This Target

AlphaFold

ADReCS ID

BADD_A05962

HIT2.0 ID

T43DMF

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 5 Approved Drugs

CHLOROXINE

Drug Info

Approved

Erythema

[2]

Dezocine

Drug Info

Approved

Pain

[3]

Difelikefalin

Drug Info

Approved

Pruritus

[4]

Nalbuphine

Drug Info

Approved

Pain

[5], [6]

Nalfurafine hcl

Drug Info

Approved

Uremic pruritus

[2]

Clinical Trial Drug(s)

[+] 18 Clinical Trial Drugs

Asimadoline

Drug Info

Phase 3

Diarrhea-predominant irritable bowel syndrome

[7]

JNJ 67953964

Drug Info

Phase 3

Major depressive disorder

[8]

CR-845

Drug Info

Phase 2/3

Pain

[9]

PHN-131

Drug Info

Phase 2/3

Pain

[10]

A277

Drug Info

Phase 2

Chronic pain

[11]

Apadoline

Drug Info

Phase 2

Pain

[12]

BTRX-335140

Drug Info

Phase 2

Major depressive disorder

[13]

CR-665

Drug Info

Phase 2

Pain

[14]

Enadoline

Drug Info

Phase 2

Pain

[15], [16]

LY-2456302

Drug Info

Phase 2

Alcohol dependence

[17]

Niravoline

Drug Info

Phase 2

Pain

[18]

ORP-101

Drug Info

Phase 2

Irritable bowel syndrome

[19]

TPM-1/Morphine

Drug Info

Phase 2

Pain

[20]

AIKO-150

Drug Info

Phase 1

Opioid dependence

[21]

BRL-52656

Drug Info

Phase 1

Pain

[22]

MCP-201

Drug Info

Phase 1

Pain

[23]

PF-4455242

Drug Info

Phase 1

Bipolar disorder

[24]

SALVINORIN A

Drug Info

Phase 1

Cerebral vasospasm

[25], [26]

Discontinued Drug(s)

[+] 7 Discontinued Drugs

ADL 10-0101

Drug Info

Discontinued in Phase 2

Pain

[27]

E-2078

Drug Info

Discontinued in Phase 2

Pain

[28], [29]

R-84760

Drug Info

Discontinued in Phase 2

Pain

[30]

VP004

Drug Info

Discontinued in Phase 1

Substance use disorder

[31]

GR-89696

Drug Info

Terminated

Neurodegenerative disorder

[33], [34]

GR-94839

Drug Info

Terminated

Pain

[35]

KT-95

Drug Info

Terminated

Inflammatory bowel disease

[36]

Preclinical Drug(s)

[+] 2 Preclinical Drugs

GNTI

Drug Info

Preclinical

Obesity

[32]

LY-25582

Drug Info

Preclinical

Obesity

[32]

Mode of Action

[+] 5 Modes of Action

Inhibitor

[+] 228 Inhibitor drugs

CHLOROXINE

Drug Info

[37]

Nalfurafine hcl

Drug Info

[40]

ORP-101

Drug Info

[51]

TPM-1/Morphine

Drug Info

[52]

AIKO-150

Drug Info

[53]

SALVINORIN A

Drug Info

[57]

CLIOQUINOL

Drug Info

[37]

Dynorphin a

Drug Info

[59]

LY-25582

Drug Info

[63]

SB-213698

Drug Info

[68]

(-)-cyclorphan

Drug Info

[69]

1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol

Drug Info

[70]

1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol

Drug Info

[70]

1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol

Drug Info

[70]

1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(4-ethylphenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(4-propylphenyl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(benzyloxy)-4-phenylpiperidine

Drug Info

[70]

1-benzhydryl-4-(furan-2-yl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(pyridin-2-yl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-benzylpiperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-butylpiperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-cyclohexylpiperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-ethoxy-4-phenylpiperidine

Drug Info

[70]

1-benzhydryl-4-hexylpiperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-isopropylpiperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-m-tolylpiperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-methoxy-4-phenylpiperidine

Drug Info

[70]

1-benzhydryl-4-o-tolylpiperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-p-tolylpiperidin-4-ol

Drug Info

[71]

1-benzhydryl-4-phenyl-4-propoxypiperidine

Drug Info

[70]

1-benzhydryl-4-phenylpiperidin-4-ol

Drug Info

[72]

1-benzhydryl-4-tert-butylpiperidin-4-ol

Drug Info

[71]

12-EPI-SALVINORIN A

Drug Info

[73]

14-O-phenylpropylnaltrexone

Drug Info

[74]

17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine

Drug Info

[75]

17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine

Drug Info

[75]

17-methyl-4'-methyldihydromorphinone

Drug Info

[76]

17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate

Drug Info

[75]

2-(2-methylquinolin-4-ylamino)-N-phenylacetamide

Drug Info

[77]

2-Benzylaminomethyl-3-hydroxymorphinan

Drug Info

[75]

2-EPI-2-THIOSALVINORIN A

Drug Info

[78]

2-EPI-2-THIOSALVINORIN B

Drug Info

[78]

2-Hydroxymethyl-3-hydroxymorphinan

Drug Info

[75]

2-THIOSALVINORIN B

Drug Info

[78]

3-(1-benzylpiperidin-4-yl)-5-chloro-1H-indole

Drug Info

[79]

3-(1-benzylpiperidin-4-yloxy)benzamide

Drug Info

[80]

3-desoxy-3-carboxamidonaltrexone

Drug Info

[81]

4-(4-((phenethylamino)methyl)phenoxy)benzamide

Drug Info

[84]

4-(p-Tolyl)spiro[chromene-2,4'-piperidine]

Drug Info

[85]

4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide

Drug Info

[86]

4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol

Drug Info

[85]

4-phenyl-1-(1-phenylbutyl)piperidin-4-ol

Drug Info

[70]

4-phenyl-1-(1-phenylethyl)piperidin-4-ol

Drug Info

[70]

4-phenyl-1-(1-phenylheptyl)piperidin-4-ol

Drug Info

[70]

4-phenyl-1-(1-phenylhexyl)piperidin-4-ol

Drug Info

[70]

4-phenyl-1-(1-phenylpentyl)piperidin-4-ol

Drug Info

[70]

4-phenyl-1-(1-phenylpropyl)piperidin-4-ol

Drug Info

[70]

4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol

Drug Info

[70]

4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol

Drug Info

[70]

4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol

Drug Info

[70]

4-phenyl-4-[1H-imidazol-2-yl]-piperidine

Drug Info

[87]

4-Phenylspiro[chromene-2,4'-piperidine]

Drug Info

[85]

5-(4-((phenethylamino)methyl)phenoxy)picolinamide

Drug Info

[84]

6-(4-((benzylamino)methyl)phenoxy)nicotinamide

Drug Info

[84]

6-(4-((phenethylamino)methyl)phenoxy)nicotinamide

Drug Info

[88]

6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide

Drug Info

[88]

6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide

Drug Info

[84]

6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol

Drug Info

[89]

6-desoxonaltrexone

Drug Info

[81]

6beta-naltrexol HCl

Drug Info

[90]

8-azabicyclo[3.2.1]octan-3-yloxy-benzamide

Drug Info

[91]

8-carboxamidocyclazocine

Drug Info

[92]

ANISOCOUMARIN H

Drug Info

[93]

Benzyl derivative of M6G

Drug Info

[94]

Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate

Drug Info

[69]

BUTORPHAN

Drug Info

[98]

Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH

Drug Info

[99]

Clocinnamox

Drug Info

[74]

CYCLAZOCINE

Drug Info

[98]

CYCLORPHAN

Drug Info

[98]

C[L-Ala-D-pro-L-Phe-D-trp]

Drug Info

[100]

C[L-mTyr-D-pro-L-Phe-D-trp]

Drug Info

[100]

C[L-Phe-D-pro-L-mTyr-D-trp]

Drug Info

[100]

C[L-Phe-D-pro-L-Phe-D-trp]

Drug Info

[100]

C[L-Phe-D-pro-L-Phe-L-trp]

Drug Info

[100]

C[L-Phe-D-pro-L-Tyr(OMe)-D-trp]

Drug Info

[100]

C[L-Phe-D-pro-L-Tyr-D-trp]

Drug Info

[100]

C[L-Tyr(OMe)-D-pro-L-Phe-D-trp]

Drug Info

[100]

C[L-Tyr-D-pro-L-Phe-D-trp]

Drug Info

[100]

100

DAMGO

Drug Info

[101]

101

Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2

Drug Info

[102]

102

DEOXY SALVINORIN A

Drug Info

[103]

103

Deprotected cogener of M6G

Drug Info

[94]

104

Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2

Drug Info

[102]

105

Dimepheptanol

Drug Info

[89]

106

DM6S

Drug Info

[101]

107

Dmt-Pro-3,5Dmp-Phe-NH2

Drug Info

[106]

108

Dmt-Pro-Dmp-Phe-NH2

Drug Info

[106]

109

Dmt-Pro-Dmt-Phe-NH2

Drug Info

[106]

110

Dmt-Pro-Emp-Phe-NH2

Drug Info

[106]

111

Dmt-Pro-Imp-Phe-NH2

Drug Info

[106]

112

Dmt-Pro-Mmp-Phe-NH2

Drug Info

[106]

113

Dmt-Pro-Phe-Phe-NH2

Drug Info

[106]

114

Dmt-Pro-Tmp-Phe-NH2

Drug Info

[106]

115

DPDPE

Drug Info

[107]

116

Dynorphin(1-8)

Drug Info

[110]

117

ELAEOCARPENINE

Drug Info

[111]

118

ENDOMORPHIN 2

Drug Info

[112]

119

ENDOMORPHIN-1

Drug Info

[112]

120

ETONITAZENE

Drug Info

[114]

121

FALCARINDIOL

Drug Info

[93]

122

H-Cdp-ala-Gly-Phe-leu-OH

Drug Info

[118]

123

H-Cdp-Gly-Gly-Phe-Leu-OH

Drug Info

[118]

124

H-Cpa-Gly-Gly-Phe-Met-NH2

Drug Info

[118]

125

H-Cpa-Gly-Gly-Phe-Met-OH

Drug Info

[118]

126

H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH

Drug Info

[99]

127

H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2

Drug Info

[119]

128

H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2

Drug Info

[119]

129

H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2

Drug Info

[119]

130

H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2

Drug Info

[119]

131

H-Tyr-Gly-Gly-Phe-Met-NH2

Drug Info

[118]

132

HERKINORIN

Drug Info

[120]

133

HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2

Drug Info

[121]

134

ICI-199441

Drug Info

[122]

135

KETOCYCLAZOCINE

Drug Info

[53]

136

KNT-62

Drug Info

[40]

137

KNT-63

Drug Info

[40]

138

LOFENTANIL

Drug Info

[124]

139

M3A6S

Drug Info

[101]

140

M3IBu6S

Drug Info

[101]

141

M3P6S

Drug Info

[101]

142

M3Pr6S

Drug Info

[101]

143

M6G thiosaccharide analogue

Drug Info

[94]

144

M6S

Drug Info

[101]

145

MC-CAM

Drug Info

[125]

146

MCL-117

Drug Info

[69]

147

MCL-139

Drug Info

[69]

148

MCL-144

Drug Info

[126]

149

MCL-145

Drug Info

[69]

150

MCL-147

Drug Info

[127]

151

MCL-149

Drug Info

[127]

152

MCL-153

Drug Info

[128]

153

MCL-154

Drug Info

[128]

154

MCL-182

Drug Info

[127]

155

MCL-183

Drug Info

[127]

156

MCL-428

Drug Info

[129]

157

MCL-429

Drug Info

[129]

158

MCL-431

Drug Info

[129]

159

MCL-432

Drug Info

[129]

160

MCL-433

Drug Info

[129]

161

MCL-434

Drug Info

[129]

162

MCL-435

Drug Info

[129]

163

MCL-443

Drug Info

[129]

164

MCL-444

Drug Info

[129]

165

MCL-445

Drug Info

[127]

166

MCL-446

Drug Info

[127]

167

MCL-447

Drug Info

[127]

168

MCL-448

Drug Info

[127]

169

MCL-449

Drug Info

[129]

170

MCL-450

Drug Info

[130]

171

MCL-451

Drug Info

[130]

172

MCL-457

Drug Info

[127]

173

MCL-458

Drug Info

[127]

174

METAZOCINE

Drug Info

[53]

175

MK-1925

Drug Info

[131]

176

Morphinan Cyclic Imine analogue

Drug Info

[132]

177

MR-1029

Drug Info

[133]

178

MR-1526

Drug Info

[133]

179

MR-2034

Drug Info

[53]

180

MR-2266

Drug Info

[133]

181

N,N-diallyl[D-Pro-10]Dyn A-(1-11)

Drug Info

[134]

182

N,N-dibenzyl[D-Pro-10]Dyn A-(1-11)

Drug Info

[134]

183

N,N-diCPM[D-Pro-10]Dyn A-(1-11)

Drug Info

[134]

184

N-(17-Methylmorphinan-3-yl)-N'-phenylurea

Drug Info

[75]

185

N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea

Drug Info

[75]

186

N-allyl[D-Pro-10]Dyn A-(1-11)

Drug Info

[134]

187

N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine

Drug Info

[75]

188

N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine

Drug Info

[75]

189

N-benzyl[D-Pro-10]Dyn A-(1-11)

Drug Info

[134]

190

N-CPM[D-Pro-10]Dyn A-(1-11)

Drug Info

[134]

191

N-isobutylnoroxymorphone

Drug Info

[135]

192

NalBzOH

Drug Info

[101]

193

Naltrexone-6-alpha-ol

Drug Info

[53]

194

NORBINALTORPHIMINE

Drug Info

[137]

195

O-DESMETHYL TRAMADOL

Drug Info

[53]

196

OXYMORPHINDOLE

Drug Info

[138]

197

Oxymorphone semicarbazone hydrochloride

Drug Info

[110]

198

PHENAZOCINE

Drug Info

[53]

199

RTI-5989-23

Drug Info

[63]

200

RTI-5989-25

Drug Info

[63]

201

RTI-5989-31

Drug Info

[139]

202

Salvinicin A

Drug Info

[140]

203

SALVINICIN B

Drug Info

[140]

204

Salvinorin A (ester)

Drug Info

[103]

205

SALVINORIN B

Drug Info

[120]

206

Salvinorin B 1-ethoxyethyl ether

Drug Info

[141]

207

Salvinorin B 2,2,2-trifluoroethoxymethyl ether

Drug Info

[141]

208

Salvinorin B 2-fluoroethoxymethyl ether

Drug Info

[141]

209

Salvinorin B 2-methoxy-2-propyl ether

Drug Info

[141]

210

Salvinorin B 2-methoxyethoxymethyl ether

Drug Info

[141]

211

Salvinorin B benzyloxymethyl ether

Drug Info

[141]

212

Salvinorin B butoxymethyl ether

Drug Info

[141]

213

Salvinorin B ethoxymethyl ether

Drug Info

[141]

214

Salvinorin B fluoromethyl ether

Drug Info

[141]

215

Salvinorin B isopropoxymethyl ether

Drug Info

[141]

216

Salvinorin B methoxymethyl ether

Drug Info

[141]

217

Salvinorin B methylthiomethyl ether

Drug Info

[141]

218

Salvinorin B propoxymethyl ether

Drug Info

[141]

219

Salvinorin B tert-butoxymethyl ether

Drug Info

[141]

220

Salvinorin B tetrahydropyran-2-yl ether

Drug Info

[141]

221

SN-11

Drug Info

[68]

222

SN-23

Drug Info

[68]

223

SN-28

Drug Info

[142]

224

SPIROINDANYLOXYMORPHONE

Drug Info

[143]

225

Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH

Drug Info

[99]

226

ZYKLOPHIN

Drug Info

[121]

227

[Dcp1]Dyn A(1-11)-NH2

Drug Info

[102]

228

[Leu5]enkephalin

Drug Info

[149]

Antagonist

[+] 14 Antagonist drugs

Dezocine

Drug Info

[1]

JNJ 67953964

Drug Info

[41]

BTRX-335140

Drug Info

[44]

LY-2456302

Drug Info

[48]

GNTI

Drug Info

[32]

Beta-endorphin

Drug Info

[95]

Diprenorphine

Drug Info

[105]

Drug 7684380

Drug Info

[108]

L-685,818

Drug Info

[108]

naltriben

Drug Info

[67]

Nor-binaltorphimine dihydrochloride

Drug Info

[96]

quadazocine

Drug Info

[67]

[3H]diprenorphine

Drug Info

[146]

[U-13C]ascomycin

Drug Info

[150]

Agonist

[+] 28 Agonist drugs

Difelikefalin

Drug Info

[38]

Asimadoline

Drug Info

[7]

CR-845

Drug Info

[42]

PHN-131

Drug Info

[43]

Apadoline

Drug Info

[12]

Carfentanil

Drug Info

[45]

CR-665

Drug Info

[46]

Enadoline

Drug Info

[16], [47]

BRL-52656

Drug Info

[54]

MCP-201

Drug Info

[55]

ADL 10-0101

Drug Info

[58]

R-84760

Drug Info

[61]

Fedotozine

Drug Info

[64]

3-Methylfentanyl

Drug Info

[82]

3-Methylthiofentanyl

Drug Info

[83]

BRL 52537 hydrochloride

Drug Info

[96]

BRL 52974

Drug Info

[97]

Dihydromorphine

Drug Info

[104]

dynorphin B

Drug Info

[109]

ethyketazocine

Drug Info

[113]

ethylketocyclazocine

Drug Info

[67]

Nalorphine

Drug Info

[136]

normorphine

Drug Info

[67]

NRP290

Drug Info

[67]

spiradoline

Drug Info

[109]

tifluadom

Drug Info

[113]

U50,488H

Drug Info

[144], [145]

[3H]U69593

Drug Info

[147], [148]

Modulator

[+] 12 Modulator drugs

Nalbuphine

Drug Info

[39]

Niravoline

Drug Info

[49], [50]

PF-4455242

Drug Info

[56]

E-2078

Drug Info

[60]

GR-89696

Drug Info

[65]

GR-94839

Drug Info

[66]

KT-95

Drug Info

[67]

GR-38414

Drug Info

[115]

GR-45809

Drug Info

[116]

GR-86014

Drug Info

[117]

GR-91272

Drug Info

[117]

ICI-204448

Drug Info

[123]

Agonist

[+] 1 Agonist drugs

A277

Drug Info

[11]

Cell-based Target Expression Variations

Top

Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Drug Binding Sites of Target

Top

Ligand Name: Meclinertant

Ligand Info

Structure Description

CryoEM Structure of Inactive NTSR1 Bound to SR48692 and Nb6

PDB:7UL2

Method

Electron microscopy

Resolution

2.40 Å

Mutation

[151]

PDB Sequence

IYSKVLVTAV

⁶⁹

YLALFVVGTV

⁷⁹

GNTVTLFTLA

⁸⁹

RSTVHYHLGS

¹⁰⁷

LALSDLLTLL

¹¹⁷

LAMPVELYNF

¹²⁷

IWVHHPWAFG

¹³⁷

DAGCRGYYFL

¹⁴⁷

RDACTYATAL

¹⁵⁷

NVASLSVERY

¹⁶⁷

LAICHPFKAK

¹⁷⁷

TLMSRSRTKK

¹⁸⁷

FISAIWLASA

¹⁹⁷

LLAVPMLFTM

²⁰⁷

GEQNRSAHAG

²²⁰

GLVCTPTIHT

²³⁰

ATVKVVIQVN

²⁴⁰

TFMSFIFPMV

²⁵⁰

VISVLYTLMI

²⁶⁰

LRLKSVRLLS

²⁷⁰

GSREKDRNLR

²⁹⁹

RITRLVLAVV

³⁰⁹

IAFVVCWLPY

³¹⁹

HVRRLMFCYI

³²⁹

SWTPFLYDFY

³⁴²

HYFYMVTNAL

³⁵²

FYVSSTINPI

³⁶²

LYNLVSANFR

³⁷²

HIFLATL

Residue

Distance (Å)

TYR145

4.569

MET203

4.498

MET207

4.486

PRO226

4.802

VAL233

4.213

ILE237

3.690

ARG322

3.104

ARG323

4.020

MET325

3.814

Residue

Distance (Å)

PHE326

3.335

ILE329

3.678

TRP334

3.919

TYR339

3.705

TYR342

3.537

HIS343

3.315

PHE345

3.793

TYR346

3.574

Ligand Name: Cholesterol

Ligand Info

Structure Description

Crystal Structure of a nanobody-stabilized active state of the kappa-opioid receptor

PDB:6B73

Method

X-ray diffraction

Resolution

3.10 Å

Mutation

Yes

[152]

PDB Sequence

LGSISPAIPV

⁶⁰

IITAVYSVVF

⁷⁰

VVGLVGNSLV

⁸⁰

MFVIIRYTKM

⁹⁰

KTATNIYIFN

¹⁰⁰

LALADALVTT

¹¹⁰

TMPFQSTVYL

¹²⁰

MNSWPFGDVL

¹³⁰

CKIVLSIDYY

¹⁴⁰

NMFTSIFTLT

¹⁵⁰

MMSVDRYIAV

¹⁶⁰

CHPVKALDFR

¹⁷⁰

TPLKAKIINI

¹⁸⁰

CIWLLSSSVG

¹⁹⁰

ISAIVLGGTK

²⁰⁰

VRDVIECSLQ

²¹³

FPDDDYSWWD

²²³

LFMKICVFIF

²³³

AFVIPVLIII

²⁴³

VCYTLMILRL

²⁵³

KSVRSREKDR

²⁶⁷

NLRRITRLVL

²⁷⁷

VVVAVFVVCW

²⁸⁷

TPIHIFILVE

²⁹⁷

ALGTSHSTAA

³⁰⁸

LSSYYFCIAL

³¹⁸

GYTNSSLNPI

³²⁸

LYAFLDENFK

³³⁸

Residue

Distance (Å)

VAL284

3.583

VAL285

3.513

THR288

3.758

PRO289

3.738

ILE292

3.758

Residue

Distance (Å)

PHE293

3.603

VAL296

4.028

THR302

3.426

SER303

4.415

SER311

4.804

Click to View More Binding Site Information of This Target with Different Ligands

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function. Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006). Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database. The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017). Human Similarity Proteins Human Pathway Affiliation Biological Network Descriptors

Different Human System Profiles of Target

Top

Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.

Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).

Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.

The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017).

Human Similarity Proteins

Human Pathway Affiliation

Biological Network Descriptors

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Olfactory receptor 2M3 (OR2M3)	PF13853	24.739 (71/287)	1.69E-11
Olfactory receptor 2M7 (OR2M7)	PF13853	25.090 (70/279)	2.42E-11
Olfactory receptor 2M2 (OR2M2)	PF13853	25.442 (72/283)	3.18E-10
Olfactory receptor 2M5 (OR2M5)	PF13853	25.088 (71/283)	4.17E-10
Olfactory receptor 2T4 (OR2T4)	PF13853	22.897 (49/214)	1.61E-08
Olfactory receptor 2AG2 (OR2AG2)	PF13853	20.875 (62/297)	1.70E-08
Olfactory receptor 2C3 (OR2C3)	PF13853	24.590 (75/305)	2.16E-08
Olfactory receptor 2G6 (OR2G6)	PF13853	23.432 (71/303)	4.60E-08
Olfactory receptor 1G1 (OR1G1)	PF13853	30.081 (37/123)	7.46E-08
Olfactory receptor 2T33 (OR2T33)	PF13853	23.248 (73/314)	2.86E-07
Olfactory receptor 2T8 (OR2T8)	PF13853	24.272 (75/309)	5.54E-07
Olfactory receptor 2H1 (OR2H1)	PF13853	22.222 (72/324)	7.31E-07
Olfactory receptor 7A10 (OR7A10)	PF13853	21.595 (65/301)	1.33E-06
Olfactory receptor 7A17 (OR7A17)	PF13853	21.543 (67/311)	1.38E-06
Olfactory receptor 2A1/2A42 (OR2A1; OR2A42)	PF13853	20.202 (60/297)	1.66E-06
Olfactory receptor 2H2 (OR2H2)	PF13853	22.436 (70/312)	1.69E-06
Olfactory receptor 7A5 (OR7A5)	PF13853	23.810 (35/147)	1.90E-06
Olfactory receptor 2A14 (OR2A14)	PF13853	20.063 (64/319)	2.29E-06
Olfactory receptor 2W1 (OR2W1)	PF13853	21.136 (67/317)	2.70E-06
Olfactory receptor 1I1 (OR1I1)	PF13853	25.641 (30/117)	4.71E-06
Olfactory receptor 6S1 (OR6S1)	PF13853	24.242 (32/132)	5.13E-06
Olfactory receptor 2A25 (OR2A25)	PF13853	25.217 (29/115)	6.32E-06
Olfactory receptor 2A2 (OR2A2)	PF13853	25.620 (31/121)	6.33E-06
Olfactory receptor 52D1 (OR52D1)	PF13853	30.000 (36/120)	6.86E-06
Olfactory receptor 2AG1 (OR2AG1)	PF13853	21.262 (64/301)	1.01E-05
Olfactory receptor 4K2 (OR4K2)	PF13853	25.773 (75/291)	1.16E-05
Putative olfactory receptor 52L2 (OR52L2P)	PF13853	27.451 (28/102)	1.35E-05
Olfactory receptor 2S2 (OR2S2)	PF13853	21.875 (63/288)	1.38E-05
Olfactory receptor 6C68 (OR6C68)	PF13853	21.739 (50/230)	2.23E-05
Olfactory receptor 7D2 (OR7D2)	PF13853	22.727 (70/308)	2.39E-05
Olfactory receptor 2V1 (OR2V1)	PF13853	25.943 (55/212)	2.53E-05
Olfactory receptor 2T34 (OR2T34)	PF13853	19.288 (65/337)	2.86E-05
Olfactory receptor 2T29 (OR2T29)	PF13853	21.070 (63/299)	2.97E-05
Olfactory receptor 2T5 (OR2T5)	PF13853	21.070 (63/299)	2.97E-05
Olfactory receptor 10Q1 (OR10Q1)	PF13853	23.488 (66/281)	2.98E-05
Olfactory receptor 7G1 (OR7G1)	PF13853	27.692 (36/130)	3.54E-05
Olfactory receptor 2T3 (OR2T3)	PF13853	19.585 (66/337)	3.61E-05
Olfactory receptor 2A5 (OR2A5)	PF13853	20.455 (45/220)	3.80E-05
Olfactory receptor 7E24 (OR7E24)	PF13853	21.951 (36/164)	3.89E-05
Olfactory receptor 52E8 (OR52E8)	PF13853	31.159 (43/138)	3.90E-05
Olfactory receptor 52L1 (OR52L1)	PF13853	26.471 (27/102)	3.97E-05
Olfactory receptor 6C65 (OR6C65)	PF13853	24.312 (53/218)	4.68E-05
Olfactory receptor 4K17 (OR4K17)	PF13853	22.727 (70/308)	5.03E-05
Olfactory receptor 2T12 (OR2T12)	PF13853	21.711 (66/304)	5.05E-05
Olfactory receptor 2AK2 (OR2AK2)	PF13853	27.523 (30/109)	5.12E-05
Putative olfactory receptor 1F12P (OR1F12P)	PF13853	29.464 (33/112)	5.43E-05
Olfactory receptor 2AT4 (OR2AT4)	PF13853	25.397 (32/126)	5.83E-05
Olfactory receptor 2T2 (OR2T2)	PF13853	23.318 (52/223)	6.05E-05
Olfactory receptor 2V2 (OR2V2)	PF13853	28.972 (31/107)	8.14E-05
Olfactory receptor 7G2 (OR7G2)	PF13853	25.000 (31/124)	9.79E-05
Olfactory receptor 51E2 (OR51E2)	PF13853	25.658 (39/152)	1.01E-04
Olfactory receptor 14I1 (OR14I1)	PF13853	26.441 (78/295)	1.10E-04
Olfactory receptor 2T10 (OR2T10)	PF13853	22.772 (46/202)	1.25E-04
Olfactory receptor 4E1 (OR4E1)	PF13853	28.037 (30/107)	1.35E-04
Olfactory receptor 1M1 (OR1M1)	PF13853	21.831 (31/142)	1.38E-04
Olfactory receptor 52B6 (OR52B6)	PF13853	30.000 (42/140)	1.40E-04
Olfactory receptor 2T11 (OR2T11)	PF13853	21.739 (65/299)	1.42E-04
Olfactory receptor 13C4 (OR13C4)	PF13853	21.824 (67/307)	1.61E-04
Olfactory receptor 5AC1 (OR5AC1)	PF13853	26.549 (30/113)	1.64E-04
Olfactory receptor 2C1 (OR2C1)	PF13853	23.077 (48/208)	1.66E-04
Olfactory receptor 6V1 (OR6V1)	PF13853	24.752 (25/101)	1.79E-04
Olfactory receptor 2M4 (OR2M4)	PF13853	26.316 (55/209)	1.79E-04
Olfactory receptor 1J4 (OR1J4)	PF13853	25.610 (42/164)	2.16E-04
Olfactory receptor 2T35 (OR2T35)	PF13853	24.107 (54/224)	2.21E-04
Putative olfactory receptor 10D4 (OR10D4P)	PF13853	26.471 (27/102)	2.72E-04
Olfactory receptor 2G3 (OR2G3)	PF13853	23.875 (69/289)	2.79E-04
Olfactory receptor 51T1 (OR51T1)	PF13853	25.521 (49/192)	3.02E-04
Olfactory receptor 52H1 (OR52H1)	PF13853	21.600 (27/125)	3.37E-04
Olfactory receptor 5K4 (OR5K4)	PF13853	27.586 (32/116)	3.37E-04
Putative olfactory receptor 2B3 (OR2B3)	PF13853	22.917 (66/288)	3.39E-04
Olfactory receptor 10H2 (OR10H2)	PF13853	24.786 (29/117)	3.51E-04
Olfactory receptor 52B4 (OR52B4)	PF13853	24.540 (40/163)	3.75E-04
Olfactory receptor 2AJ1 (OR2AJ1)	PF13853	26.168 (28/107)	3.82E-04
Olfactory receptor 1J1 (OR1J1)	PF13853	29.060 (34/117)	4.11E-04
Olfactory receptor 11H2 (OR11H2)	PF13853	19.003 (61/321)	4.58E-04
Olfactory receptor 1D4 (OR1D4)	PF13853	25.309 (41/162)	5.00E-04
Olfactory receptor 10G8 (OR10G8)	PF13853	24.638 (34/138)	5.18E-04
Olfactory receptor 13J1 (OR13J1)	PF13853	25.225 (28/111)	5.47E-04
Olfactory receptor 10H4 (OR10H4)	PF13853	25.641 (30/117)	5.48E-04
Olfactory receptor 6C76 (OR6C76)	PF13853	20.317 (64/315)	5.62E-04
Olfactory receptor 7D4 (OR7D4)	PF13853	20.690 (30/145)	5.88E-04
Olfactory receptor 52E4 (OR52E4)	PF13853	26.667 (28/105)	6.09E-04
Olfactory receptor 10G4 (OR10G4)	PF13853	22.628 (31/137)	6.18E-04
Olfactory receptor 1E2 (OR1E2)	PF13853	25.217 (29/115)	7.02E-04
Olfactory receptor 10G7 (OR10G7)	PF13853	23.358 (32/137)	7.39E-04
Olfactory receptor 1J2 (OR1J2)	PF13853	25.503 (38/149)	7.49E-04
Olfactory receptor 1E1 (OR1E1)	PF13853	22.628 (31/137)	7.51E-04
Olfactory receptor 14J1 (OR14J1)	PF13853	23.846 (31/130)	8.06E-04
Olfactory receptor 2K2 (OR2K2)	PF13853	25.000 (30/120)	1.00E-03
Olfactory receptor 51M1 (OR51M1)	PF13853	21.502 (63/293)	1.00E-03
Olfactory receptor 5K2 (OR5K2)	PF13853	22.807 (26/114)	1.00E-03
Olfactory receptor 52E6 (OR52E6)	PF13853	30.435 (42/138)	1.00E-03
Olfactory receptor 10H1 (OR10H1)	PF13853	24.771 (27/109)	1.00E-03
Olfactory receptor 13A1 (OR13A1)	PF13853	23.026 (35/152)	1.00E-03
Olfactory receptor 13G1 (OR13G1)	PF13853	23.741 (33/139)	1.00E-03
Olfactory receptor 14C36 (OR14C36)	PF13853	23.636 (26/110)	1.00E-03
Olfactory receptor 2AE1 (OR2AE1)	PF13853	29.293 (29/99)	1.00E-03
Olfactory receptor 1D2 (OR1D2)	PF13853	22.393 (73/326)	1.00E-03
Olfactory receptor 3A1 (OR3A1)	PF13853	22.050 (71/322)	1.00E-03
Putative olfactory receptor 2I1 (OR2I1P)	PF13853	23.448 (34/145)	1.00E-03
Olfactory receptor 1P1 (OR1P1)	PF13853	22.581 (63/279)	1.00E-03
Olfactory receptor 1D5 (OR1D5)	PF13853	25.309 (41/162)	1.00E-03
Olfactory receptor 2A12 (OR2A12)	PF13853	21.930 (25/114)	1.00E-03
Olfactory receptor 2B2 (OR2B2)	PF13853	22.951 (70/305)	1.00E-03
Olfactory receptor 51F1 (OR51F1)	PF13853	22.754 (38/167)	1.00E-03
Olfactory receptor 7C1 (OR7C1)	PF13853	20.395 (31/152)	2.00E-03
Olfactory receptor 10G9 (OR10G9)	PF13853	22.628 (31/137)	2.00E-03
Olfactory receptor 5K1 (OR5K1)	PF13853	22.609 (26/115)	2.00E-03
Olfactory receptor 2T6 (OR2T6)	PF13853	25.243 (26/103)	2.00E-03
Olfactory receptor 2D2 (OR2D2)	PF13853	28.000 (28/100)	2.00E-03
Olfactory receptor 52N4 (OR52N4)	PF13853	23.077 (33/143)	2.00E-03
Olfactory receptor 13C9 (OR13C9)	PF13853	23.729 (28/118)	2.00E-03
Olfactory receptor 2Z1 (OR2Z1)	PF13853	25.641 (30/117)	2.00E-03
Olfactory receptor 2A4 (OR2A4)	PF13853	23.967 (29/121)	2.00E-03
Olfactory receptor 5M11 (OR5M11)	PF13853	26.119 (35/134)	3.00E-03
Olfactory receptor 2A7 (OR2A7)	PF13853	24.590 (30/122)	3.00E-03
Olfactory receptor 2D3 (OR2D3)	PF13853	25.564 (34/133)	3.00E-03
Putative olfactory receptor 7A2 (OR7A2P)	PF13853	21.154 (66/312)	3.00E-03
Olfactory receptor 11A1 (OR11A1)	PF13853	21.500 (43/200)	3.00E-03
Olfactory receptor 13C2 (OR13C2)	PF13853	23.111 (52/225)	3.00E-03
Olfactory receptor 1Q1 (OR1Q1)	PF13853	25.758 (34/132)	3.00E-03
Olfactory receptor 9A2 (OR9A2)	PF13853	23.308 (31/133)	3.00E-03
Olfactory receptor 52N5 (OR52N5)	PF13853	26.994 (44/163)	4.00E-03
Olfactory receptor 1C1 (OR1C1)	PF13853	23.148 (25/108)	4.00E-03
Olfactory receptor 11H1 (OR11H1)	PF13853	20.063 (64/319)	4.00E-03
Putative olfactory receptor 3A4 (OR3A4P)	PF13853	24.194 (30/124)	4.00E-03
Olfactory receptor 5H14 (OR5H14)	PF13853	26.000 (26/100)	4.00E-03
Olfactory receptor 4C13 (OR4C13)	PF13853	23.016 (29/126)	4.00E-03
Olfactory receptor 11H12 (OR11H12)	PF13853	20.376 (65/319)	5.00E-03
Olfactory receptor 1E3 (OR1E3)	PF13853	25.600 (32/125)	5.00E-03
Olfactory receptor 4C11 (OR4C11)	PF13853	20.462 (62/303)	5.00E-03
Olfactory receptor 14A16 (OR14A16)	PF13853	24.038 (25/104)	5.00E-03
Olfactory receptor 4N5 (OR4N5)	PF13853	23.288 (34/146)	5.00E-03
Click to Show/Hide the Information of Human Similarity Proteins

KEGG Pathway	Pathway ID	Affiliated Target	Pathway Map
Neuroactive ligand-receptor interaction	hsa04080	Affiliated Target
Class: Environmental Information Processing => Signaling molecules and interaction	Pathway Hierarchy

Degree	1	Degree centrality	1.07E-04	Betweenness centrality	0.00E+00
Closeness centrality	1.51E-01	Radiality	1.20E+01	Clustering coefficient	0.00E+00
Neighborhood connectivity	2.00E+00	Topological coefficient	1.00E+00	Eccentricity	14
Download	Click to Download the Full PPI Network of This Target

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

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Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 1 KEGG Pathways

Neuroactive ligand-receptor interaction

Panther Pathway

[+] 3 Panther Pathways

Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway

Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway

Opioid prodynorphin pathway

Reactome

[+] 2 Reactome Pathways

Peptide ligand-binding receptors

G alpha (i) signalling events

WikiPathways

[+] 4 WikiPathways

GPCRs, Class A Rhodopsin-like

Peptide GPCRs

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

Top

REF 1

Pharmacological profiles of opioid ligands at kappa opioid receptors. BMC Pharmacol. 2006 Jan 25;6:3.

REF 2

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 3

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 4

FDA Approved Drug Products from FDA Official Website. 2021. Application Number: 214916.

REF 5

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1663).

REF 6

FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070692.

REF 7

Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.

REF 8

ClinicalTrials.gov (NCT05550532) A Randomized, Double-blind, Multicenter, Parallel-group, Placebo-controlled Study to Evaluate the Efficacy, Safety, and Tolerability of Aticaprant 10 mg as Adjunctive Therapy in Adult Participants With Major Depressive Disorder (MDD) With Moderate-to-severe Anhedonia and Inadequate Response to Current Antidepressant Therapy. U.S.National Institutes of Health.

REF 9

ClinicalTrials.gov (NCT02542384) A Study Evaluating the Overall Pain Relief and Safety of Intravenous (IV) CR845 in Patients Undergoing Abdominal Surgery.

REF 10

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029095)

REF 11

Clinical pipeline report, company report or official report of Klus Pharma

REF 12

Novel developments with selective, non-peptidic kappa-opioid receptor agonists. Expert Opin Investig Drugs. 1997 Oct;6(10):1351-68.

REF 13

ClinicalTrials.gov (NCT04221230) Study in Major Depressive Disorder With BTRX-335140 vs Placebo. U.S. National Institutes of Health.

REF 14

Effect of a kappa-opioid agonist, i.v. JNJ-38488502, on sensation of colonic distensions in healthy male volunteers. Neurogastroenterol Motil. 2009 Mar;21(3):281-90.

REF 15

REF 16

Enadoline, a selective kappa-opioid receptor agonist shows potent antihyperalgesic and antiallodynic actions in a rat model of surgical pain. Pain. 1999 Mar;80(1-2):383-9.

REF 17

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 18

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003260)

REF 19

ClinicalTrials.gov (NCT04129619) A Double-Blind, Placebo-Controlled, Phase 2, Responsive Adaptive Randomization Study of ORP-101 in Patients With Irritable Bowel Syndrome With Diarrhea (IBS-D). U.S.National Institutes of Health.

REF 20

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023017)

REF 21

ClinicalTrials.gov (NCT00829777) Safety Study of Intravenous 6 Naltrexol (AIKO-150) in Opioid-Dependent Subjects. U.S. National Institutes of Health.

REF 22

Opiate receptors within the blood-brain barrier mediate kappa agonist-induced water diuresis. J Pharmacol Exp Ther. 1993 Jul;266(1):164-71.

REF 23

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018011)

REF 24

ClinicalTrials.gov (NCT00988949) Proof Of Mechanism Study To Determine Efficacy Of PF-04455242 In Blocking Spiradoline (PF-00345768) Stimulated Prolactin Release. U.S. National Institutes of Health.

REF 25

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 26

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 27

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011770)

REF 28

REF 29

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003061)

REF 30

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005881)

REF 31

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025668)

REF 32

Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.

REF 33

REF 34

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003263)

REF 35

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003733)

REF 36

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007966)

REF 37

In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.

REF 38

Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)

REF 39

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.

REF 40

Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4.

REF 41

Kappa Opioid Receptor Antagonists as Potential Therapeutics for Mood and Substance Use Disorders. Handb Exp Pharmacol. 2022;271:473-491.

REF 42

Peptide Kappa Opioid Receptor Ligands: Potential for Drug Development. AAPS J. 2009 June; 11(2): 312-322.

REF 43

Nalbuphine: an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic. J Pharmacol Exp Ther. 1988 Jan;244(1):391-402.

REF 44

Clinical pipeline report, company report or official report of BlackThorn Therapeutics.

REF 45

Wax PM, Becker CE, Curry SC: Unexpected gas casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5.

REF 46

Analgesic efficacy of peripheral kappa-opioid receptor agonist CR665 compared to oxycodone in a multi-modal, multi-tissue experimental human pain model: selective effect on visceral pain. Anesthesiology. 2009 Sep;111(3):616-24.

REF 47

Analysis of [3H]bremazocine binding in single and combinatorial opioid receptor knockout mice. Eur J Pharmacol. 2001 Mar 2;414(2-3):189-95.

REF 48

LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders. Neuropharmacology. 2014 Feb;77:131-44.

REF 49

Effect of niravoline (RU51599), a kappa-opioid receptor agonist, on tumour-origin brain oedema. Acta Neurochir (Wien). 1999;141(7):771-8.

REF 50

Effects of niravoline (RU 51599), a selective kappa-opioid receptor agonist on intracranial pressure in gradually expanding extradural mass lesion. J Neurotrauma. 1998 Feb;15(2):117-24.

REF 51

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2023. Adis Insight

REF 52

Molecular Mechanisms of Opioid Receptor-Dependent Signaling and Behavior. Anesthesiology. 2011 December; 115(6): 1363-1381.

REF 53

Syntheses and opioid receptor binding properties of carboxamido-substituted opioids. Bioorg Med Chem Lett. 2009 Jan 1;19(1):203-8.

REF 54

Kappa-opioid receptors behind the blood-brain barrier are involved in the anti-hypertensive effects of systemically administered kappa-agonists in the conscious spontaneously hypertensive rat. J Pharm Pharmacol. 1999 Nov;51(11):1251-6.

REF 55

US patent application no. 6,924,288, Enantiomerically pure opioid diarylmethylpiperzine and methods of using same.

REF 56

Design and discovery of a selective small molecule opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242). J Med Chem. 2011 Aug 25;54(16):5868-77.

REF 57

Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor. J Med Chem. 2008 Mar 27;51(6):1824-30.

REF 58

Analgesia from a peripherally active kappa-opioid receptor agonist in patients with chronic pancreatitis. Pain. 2003 Jan;101(1-2):89-95.

REF 59

Use of receptor chimeras to identify small molecules with high affinity for the dynorphin A binding domain of the kappa opioid receptor. Bioorg Med Chem Lett. 2008 Jun 15;18(12):3667-71.

REF 60

Systemic effects of E-2078, a stabilized dynorphin A(1-8) analog, in rhesus monkeys. Psychopharmacology (Berl). 1999 Apr;143(2):190-6.

REF 61

Effects of R-84760, a selective kappa-opioid receptor agonist, on nociceptive reflex in isolated neonatal rat spinal cord. Eur J Pharmacol. 1998 Feb 19;343(2-3):171-7.

REF 62

WO patent application no. 2007,0677,14, Treatment of sequelae of psychiatric disorders.

REF 63

Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)p... J Med Chem. 1998 May 21;41(11):1980-90.

REF 64

Irritable bowel syndrome neuropharmacology. A review of approved and investigational compounds. J Clin Gastroenterol. 2002 Jul;35(1 Suppl):S58-67.

REF 65

[(11)C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers. Nucl Med Biol. 2002 Jan;29(1):47-53.

REF 66

GR94839, a kappa-opioid agonist with limited access to the central nervous system, has antinociceptive activity. Br J Pharmacol. 1992 Aug;106(4):783-9.

REF 67

REF 68

Design and synthesis of novel delta opioid receptor agonists and their pharmacologies. Bioorg Med Chem Lett. 2009 May 15;19(10):2792-5.

REF 69

Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opio... J Med Chem. 2006 Jan 12;49(1):256-62.

REF 70

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3023-7. Epub 2007 Mar 23.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1.

REF 71

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3028-33. Epub 2007 Mar 21.Synthesis and structure-activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 2.

REF 72

The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety. Bioorg Med Chem Lett. 2009 May 1;19(9):2519-23.

REF 73

Modification of the furan ring of salvinorin A: identification of a selective partial agonist at the kappa opioid receptor. Bioorg Med Chem. 2009 Feb 1;17(3):1370-80.

REF 74

14 beta-O-cinnamoylnaltrexone and related dihydrocodeinones are mu opioid receptor partial agonists with predominant antagonist activity. J Med Chem. 2009 Mar 26;52(6):1553-7.

REF 75

Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors. J Med Chem. 2010 Jan 14;53(1):402-18.

REF 76

Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorp... J Med Chem. 2006 Aug 24;49(17):5333-8.

REF 77

Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic ... Bioorg Med Chem. 2009 Aug 15;17(16):5782-90.

REF 78

Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2229-32.

REF 79

3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8.

REF 80

Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5847-52.

REF 81

Syntheses of novel high affinity ligands for opioid receptors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2289-94.

REF 82

Subramanian G, Paterlini MG, Portoghese PS, Ferguson DM: Molecular docking reveals a novel binding site model for fentanyl at the mu-opioid receptor. J Med Chem. 2000 Feb 10;43(3):381-91.

REF 83

You HJ, Colpaert FC, Arendt-Nielsen L: The novel analgesic and high-efficacy 5-HT1A receptor agonist F 13640 inhibits nociceptive responses, wind-up, and after-discharges in spinal neurons and withdrawal reflexes. Exp Neurol. 2005 Jan;191(1):174-83.

REF 84

Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52.

REF 85

Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-4-(5-hydroxyspiro[chromene-2,4'-pipe... J Med Chem. 2008 Oct 9;51(19):5893-6.

REF 86

Spirocyclic delta opioid receptor agonists for the treatment of pain: discovery of N,N-diethyl-3-hydroxy-4-(spiro[chromene-2,4'-piperidine]-4-yl) b... J Med Chem. 2009 Sep 24;52(18):5685-702.

REF 87

4-Phenyl-4-[1H-imidazol-2-yl]-piperidine derivatives, a novel class of selective delta-opioid agonists. Bioorg Med Chem Lett. 2006 Jan 1;16(1):146-9.

REF 88

Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6.

REF 89

Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists. J Med Chem. 1981 Jul;24(7):903-6.

REF 90

Design, synthesis, and characterization of 6beta-naltrexol analogs, and their selectivity for in vitro opioid receptor subtypes. Bioorg Med Chem Lett. 2009 May 15;19(10):2811-4.

REF 91

SAR development of a series of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as kappa opioid receptor antagonists. Part 2. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5405-10.

REF 92

Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-c... Bioorg Med Chem. 2008 May 15;16(10):5653-64.

REF 93

Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors. Bioorg Med Chem. 2008 Mar 15;16(6):3218-23.

REF 94

Synthesis and in vitro biological evaluation of a carbon glycoside analogue of morphine-6-glucuronide. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1583-6.

REF 95

Beta-endorphin is a potent inhibitor of thymidine incorporation into DNA via mu- and kappa-opioid receptors in fetal rat brain cell aggregates in culture. J Neurochem. 1993 Feb;60(2):765-7.

REF 96

Kappa-opioid receptor selectivity for ischemic neuroprotection with BRL 52537 in rats. Anesth Analg. 2003 Dec;97(6):1776-83.

REF 97

The antitussive activity of delta-opioid receptor stimulation in guinea pigs. J Pharmacol Exp Ther. 2000 Feb;292(2):803-9.

REF 98

Synthesis and opioid receptor affinity of morphinan and benzomorphan derivatives: mixed kappa agonists and mu agonists/antagonists as potential pha... J Med Chem. 2000 Jan 13;43(1):114-22.

REF 99

Synthesis of stable and potent delta/mu opioid peptides: analogues of H-Tyr-c[D-Cys-Gly-Phe-D-Cys]-OH by ring-closing metathesis. J Med Chem. 2007 Jun 28;50(13):3138-42.

REF 100

Nascent structure-activity relationship study of a diastereomeric series of kappa opioid receptor antagonists derived from CJ-15,208. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3647-50.

REF 101

Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5.

REF 102

Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opio... J Med Chem. 2006 Aug 24;49(17):5382-5.

REF 103

Synthesis and in vitro evaluation of salvinorin A analogues: effect of configuration at C(2) and substitution at C(18). Bioorg Med Chem Lett. 2006 Sep 1;16(17):4679-85.

REF 104

Opiate receptor binding properties of morphine-, dihydromorphine-, and codeine 6-O-sulfate ester congeners. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4291-5.

REF 105

[6-O-methyl-11C]Diprenorphine Molecular Imaging and Contrast Agent Database (MICAD) [Internet].

REF 106

Bifunctional [2',6'-dimethyl-L-tyrosine1]endomorphin-2 analogues substituted at position 3 with alkylated phenylalanine derivatives yield potent mi... J Med Chem. 2007 Jun 14;50(12):2753-66.

REF 107

Opioid agonist and antagonist activities of morphindoles related to naltrindole. J Med Chem. 1992 Nov 13;35(23):4325-9.

REF 108

FK-506-binding protein: three-dimensional structure of the complex with the antagonist L-685,818. J Biol Chem. 1993 May 25;268(15):11335-9.

REF 109

Cloning and functional comparison of kappa and delta opioid receptors from mouse brain. Proc Natl Acad Sci U S A. 1993 Jul 15;90(14):6736-40.

REF 110

Peptides as receptor selectivity modulators of opiate pharmacophores. J Med Chem. 1986 Jul;29(7):1222-5.

REF 111

Synthesis and evaluation of opioid receptor-binding affinity of elaeocarpenine and its analogs. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1601-3.

REF 112

Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues. J Med Chem. 2004 Jan 29;47(3):735-43.

REF 113

Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands. J Pharmacol Exp Ther. 1997 Aug;282(2):676-84.

REF 114

Photoactivatable opiate derivatives as irreversible probes of the mu-opioid receptor. J Med Chem. 1990 Sep;33(9):2456-64.

REF 115

A series of novel, highly potent and selective agonists for the kappa-opioid receptor. Br J Pharmacol. 1990 Dec;101(4):944-8.

REF 116

J. Med. Chem. 1993,36, 2075-2083

REF 117

Neuroprotective actions of GR89696, a highly potent and selective kappa-opioid receptor agonist.

REF 118

Further studies of tyrosine surrogates in opioid receptor peptide ligands. Bioorg Med Chem Lett. 2007 May 1;17(9):2656-60.

REF 119

Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity. J Med Chem. 2007 Mar 22;50(6):1414-7.

REF 120

Herkinorin analogues with differential beta-arrestin-2 interactions. J Med Chem. 2008 Apr 24;51(8):2421-31.

REF 121

The effects of C-terminal modifications on the opioid activity of [N-benzylTyr(1)]dynorphin A-(1-11) analogues. J Med Chem. 2009 Nov 12;52(21):6814-21.

REF 122

Arylacetamide-derived fluorescent probes: synthesis, biological evaluation, and direct fluorescent labeling of kappa opioid receptors in mouse micr... J Med Chem. 1996 Apr 12;39(8):1729-35.

REF 123

ICI 204448: a kappa-opioid agonist with limited access to the CNS.

REF 124

Potential affinity labels for the opiate receptor based on fentanyl and related compounds. J Med Chem. 1982 Aug;25(8):913-9.

REF 125

14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid rece... J Med Chem. 2009 Nov 12;52(21):6926-30.

REF 126

Univalent and bivalent ligands of butorphan: characteristics of the linking chain determine the affinity and potency of such opioid ligands. J Med Chem. 2009 Dec 10;52(23):7389-96.

REF 127

In-vitro investigation of oxazol and urea analogues of morphinan at opioid receptors. Bioorg Med Chem. 2007 Jun 15;15(12):4106-12.

REF 128

Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1507-9.

REF 129

High-affinity carbamate analogues of morphinan at opioid receptors. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1508-11.

REF 130

New opioid designed multiple ligand from Dmt-Tic and morphinan pharmacophores. J Med Chem. 2006 Sep 7;49(18):5640-3.

REF 131

Identification of MK-1925: a selective, orally active and brain-penetrable opioid receptor-like 1 (ORL1) antagonist. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4729-32.

REF 132

Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists, Bioorg. Med. Chem. Lett. 5(24):2969-2974 (1995).

REF 133

Electrophilic gamma-lactone kappa-opioid receptor probes. Analogues of 2'-hydroxy-2-tetrahydrofurfuryl-5,9-dimethyl-6,7-benzomorphan diastereomers. J Med Chem. 1991 Aug;34(8):2438-44.

REF 134

Synthesis and opioid activity of [D-Pro10]dynorphin A-(1-11) analogues with N-terminal alkyl substitution. J Med Chem. 1997 Aug 15;40(17):2733-9.

REF 135

Synthesis of N-isobutylnoroxymorphone from naltrexone by a selective cyclopropane ring opening reaction. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4978-81.

REF 136

Apparent efficacy of kappa-opioid receptor ligands on serum prolactin levels in rhesus monkeys. Eur J Pharmacol. 1999 Nov 3;383(3):305-9.

REF 137

Synthesis of pyrrolomorphinan derivatives as kappa opioid agonists. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5035-8.

REF 138

Ligand binding to nucleic acids and proteins: Does selectivity increase with strength Eur J Med Chem. 2008 Nov;43(11):2307-15.

REF 139

Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an ... J Med Chem. 2007 Aug 9;50(16):3765-76.

REF 140

Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues. J Med Chem. 2007 Jul 26;50(15):3596-603.

REF 141

Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers. Bioorg Med Chem. 2008 Feb 1;16(3):1279-86.

REF 142

Design and synthesis of KNT-127, a -opioid receptor agonist effective by systemic administration. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6302-5.

REF 143

Aerobic oxidation of indolomorphinan without the 4,5-epoxy bridge and subsequent rearrangement of the oxidation product to spiroindolinonyl-C-normo... Bioorg Med Chem. 2009 Aug 15;17(16):5983-8.

REF 144

The selective kappa-opioid receptor agonist U50,488H attenuates voluntary ethanol intake in the rat. Behav Brain Res. 2001 May;120(2):137-46.

REF 145

Effects of kappa- and mu-opioid receptor agonists on Ca2+ channels in neuroblastoma cells: involvement of the orphan opioid receptor. Eur J Pharmacol. 1999 Aug 27;379(2-3):191-8.

REF 146

kappa-Opioid receptor in humans: cDNA and genomic cloning, chromosomal assignment, functional expression, pharmacology, and expression pattern in the central nervous system. Proc Natl Acad Sci U S A.1995 Jul 18;92(15):7006-10.

REF 147

[3H]U-69593 a highly selective ligand for the opioid kappa receptor. Eur J Pharmacol. 1985 Feb 26;109(2):281-4.

REF 148

Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane der... J Med Chem. 2010 May 27;53(10):4212-22.

REF 149

Carba-analogues of fentanyl are opioid receptor agonists. J Med Chem. 2010 Apr 8;53(7):2875-81.

REF 150

NMR studies of an FK-506 analog, [U-13C]ascomycin, bound to FK-506-binding protein. J Med Chem. 1992 Jun 26;35(13):2467-73.

REF 151

Structure determination of inactive-state GPCRs with a universal nanobody. Nat Struct Mol Biol. 2022 Dec;29(12):1188-1195.

REF 152

Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor. Cell. 2018 Jan 11;172(1-2):55-67.e15.

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