Target Information

Target General Infomation
Target ID
T58992
Former ID
TTDS00128
Target Name
Delta-type opioid receptor
Gene Name
OPRD1
Synonyms
DOR-1; Delta opioid receptor; OPRD1
Target Type
Successful
Disease Acute nonspecific diarrhea; Chronic diarrhea associated with inflammatory bowel disease [ICD10: K50, K60]
Alcohol use disorders [ICD9: 303; ICD10: F10.2]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Acute migraine [ICD9: 346; ICD10: G43]
Bladder disease [ICD10: N30-N32]
Cough [ICD9: 786.2; ICD10: R05]
Diarrhea-predominant IBS [ICD9: 564.1; ICD10: K58.0]
Ischemic heart diseases [ICD9: 410-414; ICD10: I20-I25]
Moderate-to-severe pain [ICD10: R52, G89]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Overactive bladder disorder [ICD9: 188, 596.51; ICD10: C67, N32.81]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Premature ejaculation [ICD9: 302.75; ICD10: F52.4]
Rheumatoid arthritis [ICD9: 710-719, 714; ICD10: M05-M06]
Substance dependence [ICD10: F10-F19]
Urinary incontinence [ICD9: 788.3; ICD10: N39.3, N39.4, R32]
Function
G-protein coupled receptor that functions as receptor for endogenous enkephalins and for a subset of other opioids. 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 and in opiate-mediated analgesia. Plays a role in developing analgesic tolerance to morphine.
BioChemical Class
GPCR rhodopsin
Target Validation
T58992
UniProt ID
P41143
Sequence
MEPAPSAGAELQPPLFANASDAYPSACPSAGANASGPPGARSASSLALAIAITALYSAVC
AVGLLGNVLVMFGIVRYTKMKTATNIYIFNLALADALATSTLPFQSAKYLMETWPFGELL
CKAVLSIDYYNMFTSIFTLTMMSVDRYIAVCHPVKALDFRTPAKAKLINICIWVLASGVG
VPIMVMAVTRPRDGAVVCMLQFPSPSWYWDTVTKICVFLFAFVVPILIITVCYGLMLLRL
RSVRLLSGSKEKDRSLRRITRMVLVVVGAFVVCWAPIHIFVIVWTLVDIDRRDPLVVAAL
HLCIALGYANSSLNPVLYAFLDENFKRCFRQLCRKPCGRPDPSSFSRAREATARERVTAC
TPSDGPGGGAAA
Drugs and Mode of Action
Drug(s) Butorphanol Drug Info Approved Pain [538290], [542581]
Codeine Drug Info Approved Pain [538268], [539036]
Eluxadoline Drug Info Approved Diarrhea-predominant IBS [542668], [549001]
Hydromorphone Drug Info Approved Moderate-to-severe pain [551871]
Loperamide Drug Info Approved Acute nonspecific diarrhea; Chronic diarrhea associated with inflammatory bowel disease [551871]
Oxycodone Drug Info Approved Pain [538359], [542099]
ADL-5747 Drug Info Phase 2 Pain [522936]
ADL-5859 Drug Info Phase 2 Rheumatoid arthritis [522241]
AZD-2327 Drug Info Phase 2 Anxiety disorder [522445]
Carfentanil Drug Info Phase 2 Discovery agent [524366]
Met-enkephalin Drug Info Phase 2 Pain [521637], [538991]
TPM-1/Morphine Drug Info Phase 2 Pain [548201]
Codeine Drug Info Phase 1 Cough [533409], [539036]
MCP-201 Drug Info Phase 1 Pain [547634]
MCP-202 Drug Info Phase 1 Overactive bladder disorder [547635]
BIO-306 Drug Info Preclinical Acute migraine [536497]
SoRI-9409 Drug Info Preclinical Alcohol use disorders [548793]
DPI-3290 Drug Info Discontinued in Phase 2 Pain [546854]
DYNORPHIN A Drug Info Discontinued in Phase 2 Discovery agent [538995], [546012]
TRK-851 Drug Info Discontinued in Phase 1 Cough [547332]
VP004 Drug Info Discontinued in Phase 1 Substance dependence [548458]
BIPHALIN Drug Info Terminated Discovery agent [546535]
BW 373U86 Drug Info Terminated Discovery agent [545029]
LY-255582 Drug Info Terminated Discovery agent [545880]
SB-213698 Drug Info Terminated Discovery agent [546084]
SB-219825 Drug Info Terminated Pain [546476]
SNF-9007 Drug Info Terminated Discovery agent [546204]
Inhibitor (-)-cyclorphan Drug Info [527951]
(-)-eseroline Drug Info [551355]
(-)-isoelaeocarpiline Drug Info [528442]
(H-Dmt-Tic-Glu-NH-(CH(2))(5)-CO-Dap(6DMN)-NH(2) Drug Info [528238]
1,10-bis-(Dmt-Tic-amino)decane Drug Info [527916]
1,4-bis-(Dmt-Tic-amino)butane Drug Info [527916]
1,6-bis-(Dmt-Tic-amino)hexane Drug Info [527916]
1,6-bis-(N,N-dimethyl-Dmt-Tic-NH)hexane Drug Info [527916]
1-(1,2-diphenylethyl)-4-phenylpiperidin-4-ol Drug Info [528785]
1-(2-ethoxy-1-phenylethyl)-4-phenylpiperidin-4-ol Drug Info [528785]
1-(dio-tolylmethyl)-4-phenylpiperidin-4-ol Drug Info [528785]
1-benzhydryl-4-(2-fluorophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(2-methoxyphenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(3-fluorophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(3-methoxyphenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(3-phenylpropyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-bromophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-chlorophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-fluorophenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(4-methoxyphenyl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(benzyloxy)-4-phenylpiperidine Drug Info [528785]
1-benzhydryl-4-(furan-2-yl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-(thiophen-2-yl)piperidin-4-ol Drug Info [528781]
1-benzhydryl-4-benzylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-butylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-cyclohexylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-ethoxy-4-phenylpiperidine Drug Info [528785]
1-benzhydryl-4-hexylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-m-tolylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-methoxy-4-phenylpiperidine Drug Info [528785]
1-benzhydryl-4-o-tolylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-p-tolylpiperidin-4-ol Drug Info [528781]
1-benzhydryl-4-phenyl-4-propoxypiperidine Drug Info [528785]
1-benzhydryl-4-phenylpiperidin-4-ol Drug Info [530052]
1-[3-(3-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol Drug Info [528288]
1-[3-(4-biphenyl)-(1,2,4-triazol-4-yl) ]-3-phenol Drug Info [528288]
14-O-phenylpropylnaltrexone Drug Info [529991]
17-(Cyclobutylmethyl)-N-phenylmorphinan-3-amine Drug Info [530529]
17-(Cyclopropylmethyl)-N-phenylmorphinan-3-amine Drug Info [530529]
17-methyl-4'-methyldihydromorphinone Drug Info [528375]
17-Methylmorphinan-3-yl 4-Iodophenyl Carbamate Drug Info [530529]
2-Hydroxymethyl-3-hydroxymorphinan Drug Info [530529]
3,6-bis(Dmt-Tic-NH-butyl)-2(1H)-pyrazinone Drug Info [527916]
3,6-bis(Dmt-Tic-NH-ethyl)-2(1H)-pyrazinone Drug Info [527916]
3,6-bis(Dmt-Tic-NH-methyl)-2(1H)-pyrazinone Drug Info [527916]
3,6-bis(Dmt-Tic-NH-propyl)-2(1H)-pyrazinone Drug Info [527916]
3-desoxy-3-carboxamidonaltrexone Drug Info [530013]
4-(4-((phenethylamino)methyl)phenoxy)benzamide Drug Info [528996]
4-(p-Tolyl)spiro[chromene-2,4'-piperidine] Drug Info [529689]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)benzamide Drug Info [530324]
4-(Spiro[chromene-2,4'-piperidine]-4-yl)phenol Drug Info [529689]
4-phenyl-1-(1-phenylbutyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(1-phenylheptyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(1-phenylhexyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(1-phenylpentyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(phenyl(m-tolyl)methyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(phenyl(o-tolyl)methyl)piperidin-4-ol Drug Info [528785]
4-phenyl-1-(phenyl(p-tolyl)methyl)piperidin-4-ol Drug Info [528785]
4-phenyl-4-[1H-imidazol-2-yl]-piperidine Drug Info [527810]
4-Phenylspiro[chromene-2,4'-piperidine] Drug Info [529689]
5-(4-((phenethylamino)methyl)phenoxy)picolinamide Drug Info [528996]
6-(2-phenethylisoindolin-5-yloxy)nicotinamide Drug Info [529132]
6-(4-((benzylamino)methyl)phenoxy)nicotinamide Drug Info [528996]
6-(4-((phenethylamino)methyl)phenoxy)nicotinamide Drug Info [529132]
6-(4-(2-(benzylamino)ethyl)phenoxy)nicotinamide Drug Info [529132]
6-(4-(3-(benzylamino)propyl)phenoxy)nicotinamide Drug Info [528996]
6-(Allyl-methyl-amino)-4,4-diphenyl-heptan-3-ol Drug Info [533539]
6-cinnamoyl-N-methylstephasunoline Drug Info [530876]
6-cinnamoylhernandine Drug Info [530876]
6-desoxonaltrexone Drug Info [530013]
6beta-naltrexol HCl Drug Info [530077]
8-azabicyclo[3.2.1]octan-3-yloxy-benzamide Drug Info [531109]
8-carboxamidocyclazocine Drug Info [529429]
AKNADILACTAM Drug Info [530876]
AMINOFENTANYL Drug Info [528300]
ANALOG OF DYNORPHIN A Drug Info [533889]
Antanal 1 Drug Info [529704]
Antanal 2 Drug Info [529704]
Benzyl derivative of M6G Drug Info [527461]
BIPHALIN Drug Info [530392]
Bis-((-)-N-propargylmorphinan-3-yl) sebacoylate Drug Info [527951]
BUTORPHAN Drug Info [530707]
CARBOXYFENTANYL Drug Info [529088]
CCDC 710249, HCl salt Drug Info [530013]
Cis-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info [528875]
Clocinnamox Drug Info [529991]
CYCLAZOCINE Drug Info [529871]
CYCLORPHAN Drug Info [530529]
C[L-mTyr-D-pro-L-Phe-D-trp] Drug Info [530160]
C[L-Phe-D-pro-L-mTyr-D-trp] Drug Info [530160]
C[L-Phe-D-pro-L-Phe-L-trp] Drug Info [530160]
D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2(CTAP) Drug Info [533376]
D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2(CTP) Drug Info [533376]
D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2(CTOP) Drug Info [533376]
D-PhGly-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 Drug Info [533376]
DAMGO Drug Info [551220]
Dcp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info [528376]
Delta-kappa opioid heterodimer Drug Info [527089]
DELTORPHIN Drug Info [533972]
DELTORPHIN-II Drug Info [531038]
Deprotected cogener of M6G Drug Info [527461]
DERMORPHIN Drug Info [527931]
Dhp-c[D-Cys-Gly-Phe(pNO2)-D-Cys]NH2 Drug Info [528376]
Dimepheptanol Drug Info [533539]
Dmt-Pro-3,5Dmp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Dmp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Dmt-Phe-NH2 Drug Info [528832]
Dmt-Pro-Emp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Imp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Mmp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Phe-D-1-Nal-NH2 Drug Info [528646]
Dmt-Pro-Phe-D-2-Nal-NH2 Drug Info [528646]
Dmt-Pro-Phe-Phe-NH2 Drug Info [528832]
Dmt-Pro-Tmp-Phe-NH2 Drug Info [528832]
Dmt-Pro-Trp-D-2-Nal-NH2 Drug Info [528646]
DPDPE Drug Info [551220]
DYNORPHIN A Drug Info [533889]
ELAEOCARPENINE Drug Info [530705]
ENDOMORPHIN 2 Drug Info [531092]
ENDOMORPHIN-1 Drug Info [529556]
ETONITAZENE Drug Info [531519]
FALCARINDIOL Drug Info [529238]
Grandisine C Drug Info [528442]
Grandisine D Drug Info [528442]
Grandisine F Drug Info [528442]
GUANIDINONALTRINDOLE Drug Info [526656]
H-2',6'-dimethyltyrosine-Tic-OH Drug Info [530447]
H-2',6'-dimethyltyrosine-Tic-Phe-Phe-OH Drug Info [530447]
H-Aba-ala-Gly-Phe-leu-OH Drug Info [528724]
H-Aba-ala-Gly-Phe-Met-OH Drug Info [528724]
H-Aba-Gly-Gly-Phe-Leu-OH Drug Info [528724]
H-Aba-ser-Gly-Phe-Leu-Thr-OH Drug Info [528724]
H-Apa-ala-Gly-Phe-leu-OH Drug Info [528724]
H-Cdp-ala-Gly-Phe-leu-OH Drug Info [528724]
H-Cdp-Gly-Gly-Phe-Leu-OH Drug Info [528724]
H-Cdp-ser-Gly-Phe-Leu-Thr-OH Drug Info [528724]
H-Cpa-c[pen-Gly-Phe-pen]OH Drug Info [528724]
H-Cpa-Gly-Gly-Phe-Met-NH2 Drug Info [528724]
H-Cpa-Gly-Gly-Phe-Met-OH Drug Info [528724]
H-Cxp-ala-Gly-Phe-leu-OH Drug Info [528724]
H-D-Phe-c[Cys-Tyr-DTrp-Orn-Thr-Pen]-Thr-NH2 Drug Info [529704]
H-D-Tca-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info [525699]
H-D-Tic-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info [525699]
H-D-Trp-c[Cys-Tyr-D-Trp-Arg-Thr-Pen]-Thr-NH2 Drug Info [525699]
H-Dmt-Aba-Gly-NH-CH2-Bid Drug Info [528269]
H-Dmt-Aba-Gly-NH-CH2-Ph Drug Info [528269]
H-Dmt-Aba-Gly-NH-Ph Drug Info [528269]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-NH2 Drug Info [527693]
H-Dmt-D-Arg(NO2)-Phe-Lys(Z)-OH Drug Info [527693]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-NH2 Drug Info [528621]
H-Dmt-Tic-(2R,3R)-beta-MeCha-Phe-OH Drug Info [528621]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-NH2 Drug Info [528621]
H-Dmt-Tic-(2R,3S)-beta-MeCha-Phe-OH Drug Info [528621]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-NH2 Drug Info [528621]
H-Dmt-Tic-(2S,3R)-beta-MeCha-Phe-OH Drug Info [528621]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-NH2 Drug Info [528621]
H-Dmt-Tic-(2S,3S)-beta-MeCha-Phe-OH Drug Info [528621]
H-Dmt-Tic-Asp-N(Me)-Ph Drug Info [529630]
H-Dmt-Tic-Asp-NH-Bzl Drug Info [529630]
H-Dmt-Tic-Asp-NH-Ph Drug Info [529630]
H-Dmt-Tic-D-Asp-N(Me)-Ph Drug Info [529630]
H-Dmt-Tic-D-Asp-NH-Ph Drug Info [529630]
H-Dmt-Tic-Glu-Dap(6DMN)-NH(2) Drug Info [528238]
H-Dmt-Tic-Glu-NH-(CH2)5-NH2 Drug Info [527332]
H-Dmt-Tic-Glu-NH2 Drug Info [527332]
H-Dmt-Tic-Gly-N(Me)-Ph Drug Info [529630]
H-Dmt-Tic-Gly-NH-Bzl Drug Info [529630]
H-Dmt-Tic-Gly-NH-CH2-Bid Drug Info [528269]
H-Dmt-Tic-Gly-NH-Ph Drug Info [529630]
H-Dmt-Tic-Lys(Ac)-NH-CH2-Ph Drug Info [528411]
H-Dmt-Tic-Lys(Ac)-NH-Ph Drug Info [528411]
H-Dmt-Tic-Lys(Z)-NH-CH2-Ph Drug Info [528411]
H-Dmt-Tic-Lys(Z)-NH-Ph Drug Info [528411]
H-Dmt-Tic-Lys-NH-CH2-Ph Drug Info [528411]
H-Dmt-Tic-Lys-NH-Ph Drug Info [528411]
H-Dmt-Tic-NH-(CH2)6-NH-Dmt-H Drug Info [527758]
H-Dmt-Tic-NH-(CH2)6-NH-Phe-H Drug Info [527758]
H-Dmt-Tic-NH-(CH2)6-NH-Tic-H Drug Info [527758]
H-Dmt-Tic-NH-(D)-CH[(CH2)4-NH-Z]-Bid Drug Info [528411]
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid Drug Info [529630]
H-Dmt-Tic-NH-(R)CH(CH2-COOH)-Bid(N1-Me) Drug Info [529630]
H-Dmt-Tic-NH-(S)CH(CH2-COOH)-Bid(N1-Me) Drug Info [529630]
H-Dmt-Tic-NH-CH2-Boa Drug Info [529246]
H-Dmt-Tic-NH-CH2-Bta Drug Info [529246]
H-Dmt-Tic-NH-CH2-CH2-NH2 Drug Info [529041]
H-Dmt-Tic-NH-CH2-Imid Drug Info [529246]
H-Dmt-Tic-NH-CH2-ImidPh Drug Info [529246]
H-Dmt-Tic-NH-CH2-Indl Drug Info [529246]
H-Dmt-Tic-NH-CH2-Indn Drug Info [529246]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Ac]-Bid Drug Info [528411]
H-Dmt-Tic-NH-CH[(CH2)4-NH-Z]-Bid Drug Info [528411]
H-Dmt-Tic-NH-CH[(CH2)4-NH2]-Bid Drug Info [528411]
H-Dmt-Tic-OH Drug Info [527916]
H-mCpa-ala-Gly-Phe-leu-OH Drug Info [528724]
H-mCpa-Gly-Gly-Phe-Leu-OH Drug Info [528724]
H-mCpa-ser-Gly-Phe-Leu-Thr-OH Drug Info [528724]
H-Poa-ser-Gly-Phe-Leu-Thr-OH Drug Info [528724]
H-Tyr-c[cys-Gly-Phe(p-NO2)-cys]NH2 Drug Info [528724]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]-OH Drug Info [528875]
H-Tyr-c[D-Allylgly-Gly-Phe-D-Allylgly]NH2 Drug Info [528692]
H-Tyr-c[D-Allylgly-Gly-Phe-L-Allylgly]NH2 Drug Info [528692]
H-Tyr-c[D-Cys-Gly-Phe-D-Cys]NH2 Drug Info [528692]
H-Tyr-c[D-Cys-Gly-Phe-L-Cys]NH2 Drug Info [528692]
H-Tyr-c[D-Orn-(D or L)Atc-Glu]-NH2 Drug Info [528093]
H-Tyr-c[D-Orn-Aic-Glu]-NH2 Drug Info [528093]
H-Tyr-c[pen-Gly-Phe-pen]OH Drug Info [528724]
H-Tyr-D-Ala-Gly Phe-Pro-Leu-Trp-O-3,5-Bzl(CF3)2 Drug Info [529306]
H-Tyr-D-Ala-Gly-Phe-D-Leu Drug Info [528853]
H-Tyr-D-Ala-Gly-Phe-NH-NH-(NMe)Phe-Asp-Nle-Trp-Ac Drug Info [528058]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Phe-D-Asp-D-Nle-Trp-H Drug Info [528606]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo Drug Info [528606]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Drug Info [528606]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-Boc Drug Info [528058]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Drug Info [528058]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac Drug Info [528058]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Drug Info [528058]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H Drug Info [528606]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-3,5-Bzl(CF3)2 Drug Info [529306]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NH-Bzl Drug Info [529306]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-3,5-Bzl(CF3)2 Drug Info [529306]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-NMe-Bzl Drug Info [529306]
H-Tyr-D-Ala-Gly-Phe-Pro-Leu-Trp-O-Bzl Drug Info [529306]
H-Tyr-Gly-Gly-Phe-Met-NH2 Drug Info [528724]
H-Tyr-Gly-Gly-Phe-Met-OH Drug Info [528724]
H-Tyr-NMe-D-Ala-Phe-Sar-NH2 Drug Info [529395]
H-Tyr-Pro-Dap(6DMN)-Phe-NH2 Drug Info [528238]
H-Tyr-Pro-Phe-Phe-NH-(CH2)5-(C=O)-Dap(6DMN)-NH2 Drug Info [528238]
H-Tyr-Pro-Phe-Phe-NH-CH2-CH2-NH Tic Dmt-H Drug Info [529041]
H-Tyr-Tic-Cha-Phe-OH Drug Info [528621]
H-Tyr-Tic-OH Drug Info [530447]
H-Tyr-Tic-Phe-Phe-OH Drug Info [528621]
HERKINORIN Drug Info [529401]
HTyr-Gly-Gly-Phe-Leu-Arg-Arg-lle-Arg-Pro-LysNH2 Drug Info [530428]
ICI-174864 Drug Info [528410]
ICI-199441 Drug Info [527541]
ISOELAEOCARPINE Drug Info [528801]
LOFENTANIL Drug Info [533543]
LONGANINE Drug Info [530876]
LOPHOCLADINE A Drug Info [528165]
LY-255582 Drug Info [534631]
M6G thiosaccharide analogue Drug Info [527461]
MC-CAM Drug Info [530461]
MCL-117 Drug Info [527951]
MCL-139 Drug Info [527951]
MCL-144 Drug Info [530279]
MCL-145 Drug Info [527951]
MCL-147 Drug Info [528787]
MCL-149 Drug Info [528787]
MCL-153 Drug Info [530707]
MCL-154 Drug Info [530707]
MCL-182 Drug Info [528787]
MCL-183 Drug Info [528787]
MCL-428 Drug Info [528655]
MCL-429 Drug Info [528655]
MCL-431 Drug Info [528655]
MCL-432 Drug Info [528655]
MCL-433 Drug Info [528655]
MCL-434 Drug Info [528655]
MCL-435 Drug Info [528655]
MCL-443 Drug Info [528655]
MCL-444 Drug Info [528655]
MCL-445 Drug Info [528787]
MCL-446 Drug Info [528787]
MCL-447 Drug Info [528787]
MCL-448 Drug Info [528787]
MCL-449 Drug Info [528655]
MCL-450 Drug Info [528412]
MCL-451 Drug Info [528412]
MCL-458 Drug Info [528787]
METAZOCINE Drug Info [529816]
N-(17-Methylmorphinan-3-yl)-N'-phenylurea Drug Info [530529]
N-(4-Iodophenyl)-N'-(17-methylmorphinan-3-yl)urea Drug Info [530529]
N-alpha-amidino-Tyr(Me)-Pro-Trp-p-Cl-Phe-NH2 Drug Info [528594]
N-alpha-amidino-Tyr(Me)-Pro-Trp-Phe-NH2 Drug Info [528594]
N-Benzyl-17-(cyclobutylmethyl)morphinan-3-amine Drug Info [530529]
N-Benzyl-17-(cyclopropylmethyl)morphinan-3-amine Drug Info [530529]
N-methylstephisoferulin Drug Info [530876]
N-methylstephuline Drug Info [530876]
Naltrexone-6-alpha-ol Drug Info [529816]
Naltrexone-6-beta-ol Drug Info [529816]
NORBINALTORPHIMINE Drug Info [526656]
O-DESMETHYL TRAMADOL Drug Info [529816]
OXYMORPHINDOLE Drug Info [529414]
PERIPENTADENINE Drug Info [529173]
PHENAZOCINE Drug Info [529816]
PROSTEPHABYSSINE Drug Info [530876]
RTI-5989-23 Drug Info [534631]
RTI-5989-25 Drug Info [534631]
RTI-5989-31 Drug Info [528947]
SALVINORIN A Drug Info [529401]
SB-0304 Drug Info [529395]
SB-213698 Drug Info [530073]
SN-11 Drug Info [530073]
SN-23 Drug Info [530073]
SN-28 Drug Info [531165]
SNF-9007 Drug Info [528193]
SOMATOSTATIN Drug Info [533376]
TPM-1/Morphine Drug Info [544320]
Trans-H-Tyr-c[D-AllylGly-Gly-Phe-D-Allylgly]-OH Drug Info [528875]
Tyr-(NMe)Ala-L-Phe-D-Pro-NH2 Drug Info [534004]
Tyr-(R)-Aba-Gly-Phe-NH2 Drug Info [529202]
Tyr-(S)-Aba-Gly-Phe-NH2 Drug Info [529202]
Tyr-(S)-spiro-Aba-Gly-Phe-NH2 Drug Info [529202]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Ala-Gly-Phe-Met-NH2 Drug Info [530392]
Tyr-D-Ala-Gly-Phe-Met-Pro-Leu-Trp-NH-Bzl Drug Info [529724]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Drug Info [528058]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Ala-Phe-Asp-Val-Val-Thr[Beta-D-Glc]-Gly-NH2 Drug Info [534460]
Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2 Drug Info [533971]
Tyr-D-Ala-Phe-Gly-Tyr-Pro-Thr(Beta-D-Glc)-Gly-NH2 Drug Info [534460]
Tyr-D-Ala-Phe-Thr(-D-Glc)-Tyr-Pro-Ser-NH2 Drug Info [534460]
Tyr-D-Met-Phe-His-Leu-Met-Asp-NH2 Drug Info [533971]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [528193]
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [528193]
Tyr-Gly-Gly-Phe-c(Cys-Arg-Arg-Ile-Cys)-Arg-lys Drug Info [533889]
Tyr-Gly-Gly-Phe-leu-c(Cys-Arg-Ile-Arg-Cys)-lys Drug Info [533889]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [528193]
Tyr-Pro-3,5Dmp-Phe-NH2 Drug Info [528832]
Tyr-Pro-D-Phe-D-Pro-NH2 Drug Info [534004]
Tyr-Pro-D-Phe-Pro-NH2 Drug Info [534004]
Tyr-Pro-D-Phg-Phe-NH2 Drug Info [528190]
Tyr-Pro-Dmp-Phe-NH2 Drug Info [528832]
Tyr-Pro-Dmt-Phe-NH2 Drug Info [528832]
Tyr-Pro-Emp-Phe-NH2 Drug Info [528832]
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info [528193]
Tyr-Pro-Imp-Phe-NH2 Drug Info [528832]
Tyr-Pro-L-(NMe)Phe-D-Pro-NH2 Drug Info [534004]
Tyr-Pro-L-(NMe)Phe-Pro-NH2 Drug Info [534004]
Tyr-Pro-L-Phe-D-Pro-NH2 Drug Info [534004]
Tyr-Pro-L-Phe-Pro-NH2 Drug Info [534004]
Tyr-Pro-Mmp-Phe-NH Drug Info [528832]
Tyr-Pro-Phe-Phe-N(CH3)2 Drug Info [529480]
Tyr-Pro-Phe-Phe-NHCH3 Drug Info [529480]
Tyr-Pro-Phe-Phe-NHNH2 Drug Info [529480]
Tyr-Pro-Phe-Phe-OC(CH3)3 Drug Info [529480]
Tyr-Pro-Phe-Phe-OCH2CH3 Drug Info [529480]
Tyr-Pro-Phe-Phe-OCH2OH Drug Info [529480]
Tyr-Pro-Phe-Phe-OCH3 Drug Info [529480]
Tyr-Pro-Tmp-Phe-NH Drug Info [528832]
UFP-502 Drug Info [531038]
UFP-512 Drug Info [531038]
[Dcp1]Dyn A(1-11)-NH2 Drug Info [528376]
[Leu5]enkephalin Drug Info [530780]
Agonist 3-Methylfentanyl Drug Info [551402]
3-Methylthiofentanyl Drug Info [551408]
ADL-5747 Drug Info [543762]
ADL-5859 Drug Info [543762]
ARD-412 Drug Info [543762]
AZD-2327 Drug Info [531414]
BBI-11008 Drug Info [543762]
Beta-endorphin Drug Info [537660]
BIO-306 Drug Info [536497]
Butorphanol Drug Info [536098]
BW 373U86 Drug Info [535207]
Carfentanil Drug Info [551406]
Codeine Drug Info [536098]
DADLE Drug Info [535092]
Dihydromorphine Drug Info [551379]
Dimethylthiambutene Drug Info [551393]
DPI-221 Drug Info [543762]
DPI-3290 Drug Info [525347]
DSLET Drug Info [543762]
DSTBULET Drug Info [533358]
dynorphin B Drug Info [543762]
ethyketazocine Drug Info [534018]
ethylketocyclazocine Drug Info [543762]
Etorphine Drug Info [535235]
Leu-enkephalin Drug Info [535152]
MCP-201 Drug Info [550920]
MCP-202 Drug Info [547636]
MCP-203 Drug Info [543762]
MCP-204 Drug Info [543762]
MCP-205 Drug Info [543762]
Met-enkephalin Drug Info [537870]
normorphine Drug Info [543762]
NRP290 Drug Info [543762]
Oxycodone Drug Info [536427]
SB 227122 Drug Info [534953]
SNC-80 Drug Info [534994], [535449]
Tonazocine mesylate Drug Info [534994]
[3H]diprenorphine Drug Info [543762]
Antagonist 7-benzylidenenaltrexone Drug Info [535501]
CTAP Drug Info [543762]
Diprenorphine Drug Info [551387]
ICI 154129 Drug Info [537722]
naltriben Drug Info [529508]
Naltrindole Drug Info [535501]
quadazocine Drug Info [543762]
SoRI-9409 Drug Info [526028]
TIP Drug Info [534987]
TIPP Drug Info [534987]
TIPPpsi Drug Info [533937]
TRK-851 Drug Info [529642], [551871]
[3H]naltriben Drug Info [534682]
[3H]naltrindole Drug Info [526730]
Modulator Eluxadoline Drug Info
SB-219825 Drug Info [526061]
Binder Hydromorphone Drug Info [535919]
Loperamide Drug Info [537797]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway cGMP-PKG signaling pathway
Sphingolipid signaling pathway
Neuroactive ligand-receptor interaction
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway
Enkephalin release
Opioid proenkephalin pathway
Opioid proopiomelanocortin pathway
Reactome Peptide ligand-binding receptors
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
References
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Ref 538359FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 085910.
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Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525347DPI-3290 [(+)-3-((alpha-R)-alpha-((2S,5R)-4-Allyl-2,5-dimethyl-1-piperazinyl)-3-hydroxybenzyl)-N-(3-fluorophenyl)-N-methylbenzamide]. II. A mixed opioid agonist with potent antinociceptive activity and limited effects on respiratory function. J Pharmacol Exp Ther. 2003 Dec;307(3):1227-33. Epub 2003 Oct 8.
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Ref 528165J Nat Prod. 2006 Apr;69(4):640-4.Lophocladines, bioactive alkaloids from the red alga Lophocladia sp.
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Ref 528646J Med Chem. 2007 Feb 8;50(3):512-20.Synthesis and characterization of potent and selective mu-opioid receptor antagonists, [Dmt(1), D-2-Nal(4)]endomorphin-1 (Antanal-1) and [Dmt(1), D-2-Nal(4)]endomorphin-2 (Antanal-2).
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Ref 528853J Med Chem. 2007 Jun 14;50(12):2779-86. Epub 2007 May 22.Design, synthesis, and biological evaluation of novel bifunctional C-terminal-modified peptides for delta/mu opioid receptor agonists and neurokinin-1 receptor antagonists.
Ref 528875J Med Chem. 2007 Jun 28;50(13):3138-42. Epub 2007 Jun 1.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.
Ref 528947J Med Chem. 2007 Aug 9;50(16):3765-76. Epub 2007 Jul 11.Probes for narcotic receptor mediated phenomena. 34. Synthesis and structure-activity relationships of a potent mu-agonist delta-antagonist and an exceedingly potent antinociceptive in the enantiomeric C9-substituted 5-(3-hydroxyphenyl)-N-phenylethylmorphan series.
Ref 528996Bioorg Med Chem Lett. 2007 Oct 1;17(19):5349-52. Epub 2007 Aug 11.Structure-activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 1.
Ref 529041Bioorg Med Chem. 2007 Nov 15;15(22):6876-81. Epub 2007 Aug 29.A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.
Ref 529088J Med Chem. 2007 Nov 1;50(22):5528-32. Epub 2007 Oct 10.Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
Ref 529132Bioorg Med Chem Lett. 2007 Dec 15;17(24):6841-6. Epub 2007 Oct 17.Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Ref 529173J Nat Prod. 2007 Dec;70(12):1946-50. Epub 2007 Nov 27.Alkaloids with human delta-opioid receptor binding affinity from the Australian rainforest tree Peripentadenia mearsii.
Ref 529202J Med Chem. 2008 Jan 10;51(1):173-7. Epub 2007 Dec 7.Endomorphin-2 with a beta-turn backbone constraint retains the potent micro-opioid receptor agonist properties.
Ref 529238Bioorg Med Chem. 2008 Mar 15;16(6):3218-23. Epub 2007 Dec 31.Novel coumarin glycoside and phenethyl vanillate from Notopterygium forbesii and their binding affinities for opioid and dopamine receptors.
Ref 529246Bioorg Med Chem. 2008 Mar 15;16(6):3032-8. Epub 2007 Dec 23.Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
Ref 529306J Med Chem. 2008 Mar 13;51(5):1369-76. Epub 2008 Feb 12.A structure-activity relationship study and combinatorial synthetic approach of C-terminal modified bifunctional peptides that are delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Ref 529395J Med Chem. 2008 Apr 24;51(8):2571-4. Epub 2008 Mar 28.Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
Ref 529401J Med Chem. 2008 Apr 24;51(8):2421-31. Epub 2008 Apr 2.Herkinorin analogues with differential beta-arrestin-2 interactions.
Ref 529414Eur J Med Chem. 2008 Nov;43(11):2307-15. Epub 2008 Feb 29.Ligand binding to nucleic acids and proteins: Does selectivity increase with strength?.
Ref 529429Bioorg Med Chem. 2008 May 15;16(10):5653-64. Epub 2008 Mar 30.Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
Ref 529480Bioorg Med Chem. 2008 Jun 15;16(12):6415-22. Epub 2008 May 3.Structure-activity study of endomorphin-2 analogs with C-terminal modifications by NMR spectroscopy and molecular modeling.
Ref 529508Differential antagonism of delta opioid agonists by naltrindole and its benzofuran analog (NTB) in mice: evidence for delta opioid receptor subtypes. J Pharmacol Exp Ther. 1991 May;257(2):676-80.
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