Target General Infomation
Target ID
T27812
Former ID
TTDC00255
Target Name
Sodium-dependent serotonin transporter
Gene Name
SLC6A4
Synonyms
5HT transporter; 5HTT; Solute carrier family 6 member 4; SLC6A4
Target Type
Successful
Disease Attention deficit hyperactivity disorder; Severe mood disorders [ICD9: 296, 314.00, 314.01; ICD10: F30-F39, F90]
Anesthesia; Ocular disease [ICD9:338; ICD10: R20.0, H00-H59]
Anxiety disorder [ICD9: 300, 311; ICD10: F32, F40-F42]
Attention deficit hyperactivity disorder [ICD9: 314; ICD10: F90]
Appetite suppressant [ICD code not available]
Attention deficit hyperactivity disorder; Depression; Cocaine addiction [ICD9: 303-304, 304.2, 311, 314.00, 314.01; ICD10: F10-F19, F14.2, F32, F90]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Chronic low back pain; Neuropathic pain [ICD9: 338, 356.0, 356.8, 724.2, 724.5,780; ICD10: G64, G90.0, M54, M54.5, R52, G89]
Depression; Chronic pain [ICD9: 311, 338,780; ICD10: F30-F39, R52, G89]
Depressive disorders; Neuropathic pain [ICD9:296, 710.0, 356.0, 356.8; ICD10: F30-F39, M32, G64, G90.0]
Dry cough [ICD10: R05]
Depression; Attention deficit hyperactivity disorder [ICD9: 311, 314.00, 314.01; ICD10: F30-F39, F90]
Depression [ICD9: 311; ICD10: F30-F39]
Fibromyalgia [ICD9: 729.1; ICD10: M79.7]
Fibromyalgia; Myalgia; Chemotherapyinduced emesis [ICD9: 729.1, 787; ICD10: M79.1, M79.7, R11]
Inflammatory disease [ICD9: 140-229, 147, 173, 573.3, 710-719; ICD10: C11, C44, K75.9, M00-M25]
Migraine; Obisity [ICD9: 278, 346; ICD10: E66, G43]
Major depressive disorder [ICD9: 296.2, 296.3, 710.0; ICD10: F32, F33, M32]
Major depression [ICD9: 296.2, 296.3; ICD10: F32, F33]
Mood disorder [ICD10: F30-F39]
Major depressive disorder; Menopausal staging; Vasomotor symptoms [ICD9: 296, 296.2, 296.3, 627.2; ICD10: F30-F39, F32, F33, N95.0, N95.1]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Obesity [ICD9: 278; ICD10: E66]
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89]
Premature ejaculation [ICD9: 302.75; ICD10: F52.4]
Parkinson's disease [ICD9: 332; ICD10: G20]
Smoking cessation [ICD9: 292; ICD10: F17.2]
Severe mood disorders [ICD9: 296; ICD10: F30-F39]
Schizophrenia [ICD9: 295; ICD10: F20]
Schizophrenia; Sleep maintenance insomnia [ICD9:295, 307.41, 307.42, 327.0, 780.51, 780.52; ICD10: F20, F51.0, G47.0]
Function
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft backinto the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin and recycles it in a sodium-dependent manner.
BioChemical Class
Neurotransmitter:sodium symporter
Target Validation
T27812
UniProt ID
Sequence
METTPLNSQKQLSACEDGEDCQENGVLQKVVPTPGDKVESGQISNGYSAVPSPGAGDDTR
HSIPATTTTLVAELHQGERETWGKKVDFLLSVIGYAVDLGNVWRFPYICYQNGGGAFLLP
YTIMAIFGGIPLFYMELALGQYHRNGCISIWRKICPIFKGIGYAICIIAFYIASYYNTIM
AWALYYLISSFTDQLPWTSCKNSWNTGNCTNYFSEDNITWTLHSTSPAEEFYTRHVLQIH
RSKGLQDLGGISWQLALCIMLIFTVIYFSIWKGVKTSGKVVWVTATFPYIILSVLLVRGA
TLPGAWRGVLFYLKPNWQKLLETGVWIDAAAQIFFSLGPGFGVLLAFASYNKFNNNCYQD
ALVTSVVNCMTSFVSGFVIFTVLGYMAEMRNEDVSEVAKDAGPSLLFITYAEAIANMPAS
TFFAIIFFLMLITLGLDSTFAGLEGVITAVLDEFPHVWAKRRERFVLAVVITCFFGSLVT
LTFGGAYVVKLLEEYATGPAVLTVALIEAVAVSWFYGITQFCRDVKEMLGFSPGWFWRIC
WVAISPLFLLFIICSFLMSPPQLRLFQYNYPYWSIILGYCIGTSSFICIPTYIAYRLIIT
PGTFKERIIKSITPETPTEIPCGDIRLNAV
Drugs and Mode of Action
Drug(s) Amfepramone Drug Info Approved Obesity [536103]
Amitriptyline Drug Info Approved Depression; Chronic pain [536306], [539289], [551871]
Bupropion Drug Info Approved Smoking cessation [551871]
Chlorphentermine Hydrochloride Drug Info Approved Appetite suppressant [551871]
Citalopram Drug Info Approved Depression [536306], [542548]
Clomipramine Drug Info Approved Depression [536306], [539525]
Cocaine Drug Info Approved Anesthesia; Ocular disease [539436], [550681], [551871]
Desvenlafaxine Drug Info Approved Major depressive disorder [529941], [542166]
Dextromethorphan Polistirex Drug Info Approved Dry cough [551871]
Diethylpropion Drug Info Approved Migraine; Obisity [536661], [542170]
Duloxetine Drug Info Approved Depression [536306], [539298]
Escitalopram Drug Info Approved Major depression [551871]
Fluoxetine Drug Info Approved Depression [536661], [539300]
Fluvoxamine Drug Info Approved Depression [536120], [542200]
Levomilnacipran Drug Info Approved Fibromyalgia [530677], [542458]
Luvox Drug Info Approved Anxiety disorder [522423]
Nortriptyline Drug Info Approved Depression [536306], [539533]
Paroxetine Drug Info Approved Depression [468019], [537349]
Seroxat Drug Info Approved Depression [537349]
Sertraline Drug Info Approved Depression [468027], [536306]
Sibutramine Drug Info Approved Obesity [536710], [539665]
Tianeptine Drug Info Approved Major depressive disorder [536306], [542558], [551871]
Trazodone Drug Info Approved Depression [536306], [539351]
Ultracet Drug Info Approved Pain [536242]
Venlafaxine Drug Info Approved Depression [537533], [542345]
Vilazodone Drug Info Approved Major depressive disorder [531783], [542450]
Vortioxetine Drug Info Approved Major depressive disorder [532651], [542372]
Amitifadine Drug Info Phase 3 Obesity [527289], [528424]
Bicifadine Drug Info Phase 3 Chronic low back pain; Neuropathic pain [536374]
Dasotraline Drug Info Phase 3 Mood disorder [524969], [543060]
Desvenlafaxine Drug Info Phase 3 Major depressive disorder; Menopausal staging; Vasomotor symptoms [536580], [542166]
ITI-007 Drug Info Phase 3 Schizophrenia; Sleep maintenance insomnia [525226], [549912]
LITOXETINE Drug Info Phase 3 Mood disorder [544832]
Low dose ITI-007 Drug Info Phase 3 Schizophrenia [548546]
Lu-AA21004 Drug Info Phase 3 Mood disorder [532217]
Brasofensine Drug Info Phase 2 Parkinson's disease [526004]
CLR-3001 Drug Info Phase 2 Major depressive disorder [549113]
DA-8031 Drug Info Phase 2 Premature ejaculation [524220]
DOV 21947 Drug Info Phase 2 Severe mood disorders [536580]
Lu-AA34893 Drug Info Phase 2 Anxiety disorder [522236]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info Phase 2 Discovery agent [521857]
TD-9855 Drug Info Phase 2 Pain [533083]
AD-337 Drug Info Phase 1 Fibromyalgia; Myalgia; Chemotherapyinduced emesis [536188]
AVP-786 Drug Info Phase 1 Pain [526642], [532713]
BGC-20-1259 Drug Info Phase 1 Parkinson's disease [526830]
BL-1021 Drug Info Phase 1 Pain [523040]
GSK-1360707 Drug Info Phase 1 Major depressive disorder [523095]
SEP-228432 Drug Info Phase 1 Depressive disorders; Neuropathic pain [523795]
Dexfenfluramine Drug Info Withdrawn from market Obesity [537068]
ZIMELIDINE Drug Info Withdrawn from market Depression [533389], [533528]
DOV-216303 Drug Info Discontinued in Phase 2 Severe mood disorders [536580]
GSK372475 Drug Info Discontinued in Phase 2 Attention deficit hyperactivity disorder; Severe mood disorders [533085]
NS 2359 Drug Info Discontinued in Phase 2 Attention deficit hyperactivity disorder; Depression; Cocaine addiction [536580]
NS-2389 Drug Info Discontinued in Phase 2 Major depressive disorder [546575]
OxycoDex Drug Info Discontinued in Phase 2 Pain [547593]
R-sibutramine metabolite Drug Info Discontinued in Phase 2 Depression; Attention deficit hyperactivity disorder [536580]
SPD-473 Drug Info Discontinued in Phase 2 Mood disorder [546832]
YM-992 Drug Info Discontinued in Phase 2 Depression [546447]
NSD-644 Drug Info Discontinued in Phase 1 Neurological disease [548670]
RG-7166 Drug Info Discontinued in Phase 1 Major depressive disorder [549027]
6-nitroquipazine Drug Info Terminated Discovery agent [546005]
A-80426 Drug Info Terminated Discovery agent [546043]
HydrocoDex Drug Info Terminated Pain [526642], [532713]
Irindalone Drug Info Terminated Inflammatory disease [544636]
MOXIFETIN HYDROGEN MALEATE Drug Info Terminated Mood disorder [544967]
Inhibitor ((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine Drug Info [529620]
(+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine Drug Info [530012]
(+/-)-nantenine Drug Info [530558]
(2R,3R)-iodoreboxetine Drug Info [529666]
(2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine Drug Info [530282]
(2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine Drug Info [530282]
(2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine Drug Info [530282]
(2S,3S)-iodoreboxetine Drug Info [529666]
(cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane Drug Info [529523]
(R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info [530918]
(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info [530012]
(R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info [530012]
(R)-DULOXETINE Drug Info [529824]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info [530367]
(R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info [530367]
(R)-Norfluoxetine Drug Info [529814]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info [530012]
(S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info [530012]
(S)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info [530367]
(S)-NORDULOXETINE Drug Info [530368]
(S)-Norfluoxetine Drug Info [529814]
1-(1,2-diphenylethyl)piperazine Drug Info [528224]
1-(1,3-diphenylpropyl)piperazine Drug Info [528226]
1-(1,4-diphenylbutan-2-yl)piperazine Drug Info [528226]
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info [530918]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info [530918]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine Drug Info [530918]
1-(1-phenyl-2-(pyridin-2-yl)ethyl)piperazine Drug Info [528226]
1-(1-phenyl-2-(pyridin-4-yl)ethyl)piperazine Drug Info [528226]
1-(1-phenyl-2-o-tolylethyl)piperazine Drug Info [528224]
1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine Drug Info [530474]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info [530918]
1-(2-(2-bromophenyl)-1-phenylethyl)piperazine Drug Info [528224]
1-(2-(2-chlorophenyl)-1-phenylethyl)piperazine Drug Info [528224]
1-(2-(2-ethoxyphenyl)-1-phenylethyl)piperazine Drug Info [528224]
1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine Drug Info [528224]
1-(2-(2-fluorobenzyloxy)phenyl)piperazine Drug Info [530474]
1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine Drug Info [530918]
1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine Drug Info [528224]
1-(2-(3-fluorophenoxy)phenyl)piperazine Drug Info [530474]
1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine Drug Info [528224]
1-(2-(4-fluorophenoxy)phenyl)piperazine Drug Info [530474]
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine Drug Info [530012]
1-(2-(benzyloxy)phenyl)piperazine Drug Info [530474]
1-(2-(naphthalen-1-yl)-1-phenylethyl)piperazine Drug Info [528226]
1-(2-(naphthalen-2-yl)-1-phenylethyl)piperazine Drug Info [528226]
1-(2-(naphthalen-2-yl)ethyl)piperazine Drug Info [530012]
1-(2-(phenoxymethyl)phenyl)piperazine Drug Info [530474]
1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info [528036]
1-(2-phenoxyphenyl)piperazine Drug Info [530474]
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol Drug Info [527062]
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol Drug Info [527062]
1-(3,4-dichlorophenyl)-3-aza-bicyclo[3.1.0]hexane Drug Info [529523]
1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one Drug Info [530442]
1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info [528036]
1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info [528036]
1-(4-Benzylsulfanyl-phenyl)-propylamine Drug Info [530347]
1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info [530728]
1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info [528036]
1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info [528036]
1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info [528036]
1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info [529523]
1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info [529523]
1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info [529523]
1-benzylpiperidine hydrochloride Drug Info [528826]
1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane Drug Info [529523]
1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info [529523]
1-Methyl-2-(4-phenylsulfanyl-phenyl)-ethylamine Drug Info [530347]
1-Methyl-4-p-tolyl-piperidine-4-carbonitrile Drug Info [525662]
1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one Drug Info [528036]
1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info [529523]
10R-hydroxylobel-7-ene Drug Info [528364]
10R-hydroxylobelane Drug Info [528364]
10S-hydroxylobel-7-ene Drug Info [528364]
10S-hydroxylobelane Drug Info [528364]
1S,2R-milnacipran Drug Info [529776]
2-(2'-Aminoethyl)-5-benzyltetrahydrofuran Drug Info [529955]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info [530596]
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info [530596]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine Drug Info [530596]
2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info [528224]
2-(3-Methyl-piperazin-1-yl)-6-nitro-quinoline Drug Info [525836]
2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran Drug Info [529955]
2-(Aminomethyl)-5-(1'-naphthyl)tetrahydrofuran Drug Info [529955]
2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran Drug Info [529955]
2-(Aminomethyl)-5-phenethyltetrahydrofuran Drug Info [529955]
2-(N-Cyclopentylamino)-3'-methoxypropiophenone Drug Info [530728]
2-(N-Cyclopropylamino)-3-chloropropiophenone Drug Info [530442]
2-(N-tert-Butylamino)-3',4'-dichloropropiophenone Drug Info [530442]
2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one Drug Info [530728]
2-(tert-Butylamino)-3',4'-dichlorobutyrophenone Drug Info [530442]
2-(tert-Butylamino)-3',4'-dichloropentanophenone Drug Info [530442]
2-Amino-1-(4-ethylthiophenyl)butane Drug Info [530347]
2-Amino-1-(4-ethylthiophenyl)propane Drug Info [530347]
2-Amino-1-(4-methylthiophenyl)butane Drug Info [530347]
2-Amino-1-(4-methylthiophenyl)propane Drug Info [530347]
2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran Drug Info [529955]
2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran Drug Info [529955]
2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran Drug Info [529955]
2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran Drug Info [529955]
2-Aminomethyl-5-(phenyl)tetrahydrofuran Drug Info [529955]
2-N,N-Dimethylamino-1-(4-methylthiophenyl)propane Drug Info [530347]
2-N-(Isopropyl)amino-1-(4-methylthiophenyl)butane Drug Info [530347]
2-N-(n-Propyl)amino-1-(4-methylthiophenyl)butane Drug Info [530347]
2-N-Allylamino-1-(4-methylthiophenyl)propan Drug Info [530347]
2-N-Cyclopropylamino-1-(4-methylthiophenyl)butane Drug Info [530347]
2-N-Ethylamino-1-(4-ethylthiophenyl)butane Drug Info [530347]
2-N-Ethylamino-1-(4-ethylthiophenyl)propane Drug Info [530347]
2-N-Ethylamino-1-(4-methylthiophenyl)butane Drug Info [530347]
2-N-Ethylamino-1-(4-methylthiophenyl)propane Drug Info [530347]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)butane Drug Info [530347]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)propane Drug Info [530347]
2-N-Hydroxyamino-1-(4-methylthiophenyl)butane Drug Info [530347]
2-N-Hydroxyamino-1-(4-methylthiophenyl)propane Drug Info [530347]
2-N-Methoxyamino-1-(4-methylthiophenyl)propane Drug Info [530347]
2-N-Methylamino-1-(4-ethylthiophenyl)propane Drug Info [530347]
2-N-Methylamino-1-(4-methylthiophenyl)butane Drug Info [530347]
2-N-Methylamino-1-(4-methylthiophenyl)propane Drug Info [530347]
2-N-Propargylamino-1-(4-methylthiophenyl)butane Drug Info [530347]
2-N-Propargylamino-1-(4-methylthiophenyl)propane Drug Info [530347]
2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole Drug Info [534352]
2-phenoxy-3-(piperidin-4-yl)pyridine Drug Info [530596]
2-[1,4]Diazepan-1-yl-6-nitro-quinoline Drug Info [525836]
3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine Drug Info [529764]
3-(1H-indol-3-yl)-N,N-dimethylpropan-1-amine Drug Info [529015]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzamide Drug Info [528224]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info [528224]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info [528224]
3-(3,4-dichlorophenyl)-2-nortropene Drug Info [530502]
3-(3-aminocyclopentyl)-1H-indole-5-carbonitrile Drug Info [531220]
3-(4-Chlorophenyl)-2-nortropene Drug Info [530502]
3-(4-Fluorophenyl)-2-nortropene Drug Info [530502]
3-(4-Trifluoromethylphenyl)-2-nortropene Drug Info [530502]
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine Drug Info [530596]
3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane Drug Info [530502]
3-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info [525836]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane Drug Info [525906]
3-Phenyl-2-nortropene Drug Info [530502]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info [528473]
4-((naphthalen-2-yloxy)methyl)piperidine Drug Info [530012]
4-(1H-indol-3-yl)-N,N-dimethylcyclohex-3-enamine Drug Info [528760]
4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine Drug Info [530474]
4-(2-((dimethylamino)methyl)phenoxy)benzonitrile Drug Info [529550]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine Drug Info [530474]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine Drug Info [530474]
4-(2-(3-chlorophenoxy)phenyl)piperidine Drug Info [530474]
4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine Drug Info [530474]
4-(2-(3-fluorophenoxy)phenyl)piperidine Drug Info [530474]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine Drug Info [530474]
4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine Drug Info [530474]
4-(2-(4-fluorophenoxy)phenyl)piperidine Drug Info [530474]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine Drug Info [530474]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine Drug Info [530474]
4-(2-(benzyloxy)phenyl)piperidine Drug Info [530474]
4-(2-(phenoxymethyl)phenyl)piperidine Drug Info [530474]
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine Drug Info [530596]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine Drug Info [530474]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine Drug Info [530474]
4-(2-fluoro-6-phenoxyphenyl)piperidine Drug Info [530474]
4-(2-phenoxyphenyl)piperidine Drug Info [530474]
4-(3-fluoro-2-phenoxyphenyl)piperidine Drug Info [530474]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info [531079]
4-Allyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info [526278]
4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info [526278]
4-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info [526278]
4-Chloro-6-nitro-2-piperazin-1-yl-quinoline Drug Info [526278]
4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline Drug Info [526278]
4-Iodo-6-nitro-2-piperazin-1-yl-quinoline Drug Info [526278]
6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info [529523]
6,8-Dinitro-2-piperazin-1-yl-quinoline Drug Info [525836]
6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline Drug Info [529523]
6-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info [530012]
6-Bromo-2-piperazin-1-yl-quinoline Drug Info [525836]
6-Chloro-2-piperazin-1-yl-quinoline Drug Info [525836]
6-Iodo-2-piperazin-1-yl-quinoline Drug Info [525836]
6-Nitro-2-piperazin-1-yl-4-vinyl-quinoline Drug Info [526278]
6-Nitro-4-phenyl-2-piperazin-1-yl-quinoline Drug Info [526278]
6-nitroquipazine Drug Info [528747]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info [530012]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane Drug Info [525906]
8R-hydroxylobel-9-ene Drug Info [530601]
8R-hydroxylobelane Drug Info [528364]
8S-hydroxylobel-9-ene Drug Info [528364]
8S-hydroxylobelane Drug Info [528364]
A-80426 Drug Info [534352]
Amfepramone Drug Info [536103]
Amitifadine Drug Info [543976]
Amitriptyline Drug Info [536774], [537983]
Beta-methoxyamphetamine Drug Info [530347]
Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine Drug Info [529592]
Bupropion Drug Info [537422]
Clomipramine Drug Info [537225]
CLR-3001 Drug Info [549794]
Cocaine Drug Info [537241]
COCAINE.HCL Drug Info [528826]
Cyclohexyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info [526591]
Cyclopentyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info [526591]
D-166A Drug Info [529287]
D-211A Drug Info [529287]
D-211B Drug Info [529287]
D-254C Drug Info [529287]
D-257A Drug Info [529287]
D-257C Drug Info [529287]
DA-8031 Drug Info [532463]
Dasotraline Drug Info [533235]
Dexfenfluramine Drug Info [536335]
Diethylpropion Drug Info [536130]
DIFLUOROBENZTROPINE Drug Info [528473]
DOV 21947 Drug Info [536580]
DOV-216303 Drug Info [536580]
Duloxetine Drug Info [536331], [537531]
Erythro-3,4-dichloromethylphenidate hydrochloride Drug Info [528826]
Escitalopram Drug Info [537557]
Fluvoxamine Drug Info [537565], [537730]
GSK-1360707 Drug Info [532361]
GSK372475 Drug Info [536580]
Irindalone Drug Info [533382]
Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine Drug Info [528048]
JNJ-28583867 Drug Info [529199]
KF-A5 Drug Info [529032]
KF-A6 Drug Info [529032]
MDL-28618 Drug Info [529620]
METHYLENEDIOXYAMPHETAMINE Drug Info [530347]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info [530347]
N*1*-(6-Nitro-quinolin-2-yl)-ethane-1,2-diamine Drug Info [525836]
N,N-dimethyl(2-phenoxyphenyl)methanamine Drug Info [529278]
N-(2-oxazolemethyl)milnacipran Drug Info [529263]
N-(piperidin-4-yl)-N-propyl-2-naphthamide Drug Info [530367]
N-benzyl-N-isobutylpiperidin-4-amine Drug Info [528048]
N-cyclobutyl-N-(piperidin-4-yl)-2-naphthamide Drug Info [530367]
NISOXETINE Drug Info [529824]
norzotepine Drug Info [530783]
NS 2359 Drug Info [536499]
O-DESMETHYL TRAMADOL Drug Info [527832]
OxycoDex Drug Info [526642], [532713]
Para-chloroamphetamine Drug Info [530347]
PF-18298 Drug Info [530918]
PF-3409409 Drug Info [530265]
PF-526014 Drug Info [530918]
PYROVALERONE Drug Info [528036]
QUIPAZINE Drug Info [525836]
R-226161 Drug Info [528772]
R-NORDULOXETINE Drug Info [530368]
RG-7166 Drug Info [549028]
RTI-219 Drug Info [528932]
S-34324 Drug Info [527481]
S33005 Drug Info [536286]
SEP-228432 Drug Info [548778]
Sertraline Drug Info [536303], [536503]
SPD-473 Drug Info [527287]
TEFLUDAZINE Drug Info [533519]
Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride Drug Info [528826]
Threo-3,4-dichlororitalinol hydrochloride Drug Info [528826]
Tianeptine Drug Info [536306]
Trans-3-(o-tolyloxy)-2,3-dihydro-1H-inden-1-amine Drug Info [529530]
Ultracet Drug Info [537457]
Venlafaxine Drug Info [537422]
Vortioxetine Drug Info [532651]
WIN-35065 Drug Info [528932]
WIN-35065-2 Drug Info [534240]
WIN-35066-2 Drug Info [527309]
WIN_35428 Drug Info [534240]
YM-992 Drug Info [536286]
ZIMELIDINE Drug Info [533558]
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine Drug Info [527062]
Modulator 3,4-Methylenedioxymethamphetamine Drug Info [551382]
AD-337 Drug Info [1572591]
AVP-786 Drug Info [526642], [532713]
BGC-20-1259 Drug Info
Bicifadine Drug Info
BL-1021 Drug Info
Brasofensine Drug Info [526004]
Chlorphentermine Hydrochloride Drug Info
Citalopram Drug Info [556264]
Desvenlafaxine Drug Info [529941]
Dextromethorphan Polistirex Drug Info [556264]
Fluoxetine Drug Info [556264]
HydrocoDex Drug Info [526642], [532713]
Levomilnacipran Drug Info [530677]
LITOXETINE Drug Info
Lu-AA21004 Drug Info [531563], [532217], [532651]
Lu-AA34893 Drug Info [551828]
Luvox Drug Info [1572591]
MMDA Drug Info [551393]
Nortriptyline Drug Info [556264]
NS-2389 Drug Info [550007]
Paroxetine Drug Info [556264]
R-sibutramine metabolite Drug Info
Seroxat Drug Info [556264]
Sibutramine Drug Info [556264]
TD-9855 Drug Info [533083]
Trazodone Drug Info [556264]
Vilazodone Drug Info [531783]
Antagonist 4-Methoxyamphetamine Drug Info [551380]
ITI-007 Drug Info [551041]
Low dose ITI-007 Drug Info [551041]
Binder CX-1001 Drug Info [543976]
Activator NSD-644 Drug Info [550360]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Serotonergic synapse
NetPath Pathway TCR Signaling Pathway
PANTHER Pathway 5HT1 type receptor mediated signaling pathway
5HT2 type receptor mediated signaling pathway
5HT3 type receptor mediated signaling pathway
5HT4 type receptor mediated signaling pathway
WikiPathways Monoamine Transport
SIDS Susceptibility Pathways
NRF2 pathway
Synaptic Vesicle Pathway
Serotonin Transporter Activity
References
Ref 468019(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: 4790).
Ref 468027(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: 4798).
Ref 521857ClinicalTrials.gov (NCT00353938) Study of 3,4-Methylenedioxymethamphetamine-assisted Psychotherapy in People With Posttraumatic Stress Disorder. U.S. National Institutes of Health.
Ref 522236ClinicalTrials.gov (NCT00622245) Efficacy and Safety of Lu AA34893 in Patients With Bipolar Depression. U.S. National Institutes of Health.
Ref 522423ClinicalTrials.gov (NCT00743834) Cost-Effectiveness of Adding Web-Based Cognitive-Behavioral Therapy (CBT) to Luvox CR for Obsessive Compulsive Disorder (OCD). U.S. National Institutes of Health.
Ref 523040ClinicalTrials.gov (NCT01121380) A Study Intended to Evaluate Safety, Tolerability and Pharmacokinetics (PK) Parameters of BL-1021. U.S. National Institutes of Health.
Ref 523095ClinicalTrials.gov (NCT01153802) An Open Label Positron Emission Tomography Study in Healthy Male Subjects to Investigate Brain DAT and SERT Occupancy,Pharmacokinetics and Safety of Single Oral Dosesof GSK1360707, Using 11C- PE2I and 11C-DASB as PET Ligands. U.S. National Institutes of Health.
Ref 523795ClinicalTrials.gov (NCT01531972) A Phase 1, Open-Label, Single-photon Emission Computed Tomography (SPECT) Study to Evaluate Serotonin and Dopamine Transporter Occupancy After Multiple Dose Administration of SEP-228432 to Achieve Steady State in Healthy Subjects. U.S. National Institutes of Health.
Ref 524220ClinicalTrials.gov (NCT01798667) Clinical Trial to Evaluate the Efficacy and Safety of DA-8031 in Male Patients With Premature Ejaculation. U.S. National Institutes of Health.
Ref 524969ClinicalTrials.gov (NCT02276209) Dasotraline Adult ADHD Study. U.S. National Institutes of Health.
Ref 525226ClinicalTrials.gov (NCT02469155) A Trial to Assess the Antipsychotic Efficacy of ITI-007 Over 6 Weeks of Treatment.
Ref 526004Brasofensine NeuroSearch. Curr Opin Investig Drugs. 2000 Dec;1(4):504-7.
Ref 526642Dextromethorphan antagonizes the acute depletion of brain serotonin by p-chloroamphetamine and H75/12 in rats. Brain Res. 1992 Oct 30;594(2):323-6.
Ref 526830Pharmacological characterization of RS-1259, an orally active dual inhibitor of acetylcholinesterase and serotonin transporter, in rodents: possible treatment of Alzheimer's disease. J Pharmacol Sci.2003 Sep;93(1):95-105.
Ref 527289J Clin Pharmacol. 2004 Dec;44(12):1360-7.DOV 216,303, a "triple" reuptake inhibitor: safety, tolerability, and pharmacokinetic profile.
Ref 528424Preclinical and clinical pharmacology of DOV 216,303, a "triple" reuptake inhibitor. CNS Drug Rev. 2006 Summer;12(2):123-34.
Ref 5299412008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 532217Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats. Pharmacol Biochem Behav. 2013 Apr;105:41-50.
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 532713Antitussives and substance abuse. Subst Abuse Rehabil. 2013 Nov 6;4:75-82.
Ref 533083Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor. Int J Neuropsychopharmacol. 2014 Dec 13;18(2). pii: pyu027.
Ref 533085Pilot Phase II study of mazindol in children with attention deficit/hyperactivity disorder. Drug Des Devel Ther. 2014 Dec 1;8:2321-32.
Ref 533389The effect of zimelidine, a serotonin-reuptake blocker, on cataplexy and daytime sleepiness of narcoleptic patients. Clin Neuropharmacol. 1986;9(1):46-51.
Ref 533528Pharmacokinetic study of zimelidine using a new GLC method. Clin Pharmacokinet. 1983 Nov-Dec;8(6):530-40.
Ref 536103Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418.
Ref 536120Autism spectrum disorders: emerging pharmacotherapy. Expert Opin Emerg Drugs. 2005 Aug;10(3):521-36.
Ref 536188Emerging drugs for chemotherapy-induced emesis. Expert Opin Emerg Drugs. 2006 Mar;11(1):137-51.
Ref 536242The Diversion of Ultram, Ultracet, and generic tramadol HCL. J Addict Dis. 2006;25(2):53-8.
Ref 536306Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 536661Anti-obesity drugs and neural circuits of feeding. Trends Pharmacol Sci. 2008 Apr;29(4):208-17. Epub 2008 Mar 18.
Ref 536710Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.
Ref 537068Obesity: pathophysiology and clinical management. Curr Med Chem. 2009;16(4):506-21.
Ref 537349Emerging drug therapies in Huntington's disease. Expert Opin Emerg Drugs. 2009 Jun;14(2):273-97.
Ref 537533Desvenlafaxine in the treatment of major depressive disorder. Neuropsychiatr Dis Treat. 2009;5:127-36. Epub 2009 Apr 8.
Ref 539289(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: 200).
Ref 539298(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: 202).
Ref 539300(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: 203).
Ref 539351(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: 213).
Ref 539436(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: 2286).
Ref 539525(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: 2398).
Ref 539533(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: 2404).
Ref 539665(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: 2586).
Ref 542166(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: 7158).
Ref 542170(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: 7161).
Ref 542200(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: 7189).
Ref 542345(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: 7321).
Ref 542372(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: 7351).
Ref 542450(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: 7427).
Ref 542458(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: 7435).
Ref 542548(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: 7547).
Ref 542558(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: 7558).
Ref 543060(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: 8308).
Ref 544636Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000378)
Ref 544832Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001264)
Ref 544967Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001731)
Ref 546005Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005841)
Ref 546043Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006017)
Ref 546447Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008166)
Ref 546575Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009012)
Ref 546832Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010517)
Ref 547593Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017613)
Ref 548546Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026498)
Ref 548670Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027571)
Ref 549027Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031598)
Ref 549113Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032468)
Ref 549912Clinical pipeline report, company report or official report of Intra-Cellular Therapies.
Ref 550681Drug information of Cocaine, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 525355Moxidectin causes adult worm mortality of human lymphatic filarial parasite Brugia malayi in rodent models. Folia Parasitol (Praha). 2014 Dec;61(6):561-70.
Ref 525662Bioorg Med Chem Lett. 1999 Dec 6;9(23):3273-6.Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine.
Ref 525836Bioorg Med Chem Lett. 2000 Jul 17;10(14):1559-62.Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1.
Ref 525906Bioorg Med Chem Lett. 2000 Nov 6;10(21):2445-7.3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter.
Ref 526004Brasofensine NeuroSearch. Curr Opin Investig Drugs. 2000 Dec;1(4):504-7.
Ref 526278Bioorg Med Chem Lett. 2002 Mar 11;12(5):811-5.Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 2: 4-substituted 6-nitroquipazines.
Ref 526591J Med Chem. 2003 Apr 10;46(8):1538-45.Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate.
Ref 526642Dextromethorphan antagonizes the acute depletion of brain serotonin by p-chloroamphetamine and H75/12 in rats. Brain Res. 1992 Oct 30;594(2):323-6.
Ref 527062J Med Chem. 2004 May 6;47(10):2624-34.Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters.
Ref 527287Dopamine uptake inhibitor-induced rotation in 6-hydroxydopamine-lesioned rats involves both D1 and D2 receptors but is modulated through 5-hydroxytryptamine and noradrenaline receptors. J Pharmacol Exp Ther. 2005 Mar;312(3):1124-31. Epub 2004 Nov 12.
Ref 527309J Med Chem. 2004 Dec 2;47(25):6401-9.Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl ester isomers.
Ref 527481J Med Chem. 2005 Mar 24;48(6):2054-71.Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Ref 527832Bioorg Med Chem Lett. 2006 Feb;16(3):691-4. Epub 2005 Oct 27.Derivatives of tramadol for increased duration of effect.
Ref 528036J Med Chem. 2006 Feb 23;49(4):1420-32.1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors.
Ref 528048Bioorg Med Chem Lett. 2006 May 15;16(10):2714-8. Epub 2006 Feb 23.N-Alkyl-N-arylmethylpiperidin-4-amines: novel dual inhibitors of serotonin and norepinephrine reuptake.
Ref 528224Bioorg Med Chem Lett. 2006 Aug 15;16(16):4345-8. Epub 2006 Jun 5.N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.
Ref 528226Bioorg Med Chem Lett. 2006 Aug 15;16(16):4349-53. Epub 2006 Jun 5.Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.
Ref 528364Bioorg Med Chem Lett. 2006 Oct 1;16(19):5018-21. Epub 2006 Aug 14.Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters.
Ref 528473J Med Chem. 2006 Oct 19;49(21):6391-9.Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogues for in vivo investigation.
Ref 528747Bioorg Med Chem. 2007 May 15;15(10):3499-504. Epub 2007 Mar 3.Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2'-Substituted 6-nitroquipazines.
Ref 528760Bioorg Med Chem Lett. 2007 Jun 1;17(11):3099-104. Epub 2007 Mar 16.Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.
Ref 528772Bioorg Med Chem. 2007 Jun 1;15(11):3649-60. Epub 2007 Mar 21.Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Ref 528826J Med Chem. 2007 May 31;50(11):2718-31. Epub 2007 May 10.Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate.
Ref 528932J Med Chem. 2007 Jul 26;50(15):3686-95. Epub 2007 Jun 30.Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.
Ref 529015Bioorg Med Chem Lett. 2007 Oct 15;17(20):5647-51. Epub 2007 Aug 22.Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor.
Ref 529032Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40. Epub 2007 Sep 10.Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum.
Ref 529199Bioorg Med Chem Lett. 2008 Jan 1;18(1):39-43. Epub 2007 Nov 13.Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.
Ref 529263Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9. Epub 2008 Jan 9.Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.
Ref 529278Bioorg Med Chem Lett. 2008 Jan 15;18(2):596-9.1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity.
Ref 529287Bioorg Med Chem. 2008 Mar 15;16(6):2769-78. Epub 2008 Jan 11.Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an exocyclic hydroxyl group: interaction with dopamine, serotonin, and norepinephrine transporters.
Ref 529523Bioorg Med Chem Lett. 2008 Jul 1;18(13):3682-6. Epub 2008 May 23.Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Ref 529530Bioorg Med Chem Lett. 2008 Jul 15;18(14):4224-7. Epub 2008 May 20.Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Ref 529550Bioorg Med Chem Lett. 2008 Jul 15;18(14):4018-21. Epub 2008 Jun 5.Designing rapid onset selective serotonin re-uptake inhibitors. 2: structure-activity relationships of substituted (aryl)benzylamines.
Ref 529592Bioorg Med Chem Lett. 2008 Aug 1;18(15):4355-9. Epub 2008 Jun 25.Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.
Ref 529620Bioorg Med Chem Lett. 2008 Aug 15;18(16):4495-8. Epub 2008 Jul 17.Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.
Ref 529666Bioorg Med Chem Lett. 2008 Sep 15;18(18):4940-3. Epub 2008 Aug 19.New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter.
Ref 529764Bioorg Med Chem Lett. 2008 Dec 1;18(23):6067-70. Epub 2008 Oct 11.Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
Ref 529776J Med Chem. 2008 Nov 27;51(22):7265-72.Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.
Ref 529814Bioorg Med Chem. 2009 Jan 1;17(1):337-43. Epub 2008 Nov 5.Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression.
Ref 529824Bioorg Med Chem Lett. 2009 Jan 1;19(1):58-61. Epub 2008 Nov 13.1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors.
Ref 5299412008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
Ref 529955Bioorg Med Chem. 2009 Mar 1;17(5):2047-68. Epub 2009 Jan 15.2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors.
Ref 530012Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32. Epub 2009 Feb 20.Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1.
Ref 530265Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83. Epub 2009 Jul 2.Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template.
Ref 530282Bioorg Med Chem Lett. 2009 Sep 1;19(17):4996-8. Epub 2009 Jul 16.Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter.
Ref 530347Eur J Med Chem. 2009 Dec;44(12):4862-88. Epub 2009 Aug 6.Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents.
Ref 530367Bioorg Med Chem Lett. 2009 Oct 15;19(20):5893-7. Epub 2009 Aug 21.Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2.
Ref 530368Bioorg Med Chem. 2009 Oct 1;17(19):6890-7. Epub 2009 Aug 20.Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents fordepression.
Ref 530442J Med Chem. 2009 Nov 12;52(21):6768-81.Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction.
Ref 530474Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7. Epub 2009 Oct 12.Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
Ref 530502Bioorg Med Chem Lett. 2009 Dec 15;19(24):6865-8. Epub 2009 Oct 23.Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes.
Ref 530558Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine.
Ref 530596Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7. Epub 2009 Dec 6.Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists.
Ref 530601Bioorg Med Chem. 2010 Jan 15;18(2):640-9. Epub 2009 Dec 6.Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 530728J Med Chem. 2010 Mar 11;53(5):2204-14.Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation.
Ref 530783Norzotepine, a major metabolite of zotepine, exerts atypical antipsychotic-like and antidepressant-like actions through its potent inhibition of norepinephrine reuptake. J Pharmacol Exp Ther. 2010 Jun;333(3):772-81.
Ref 530918Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92. Epub 2010 Apr 18.Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reducing ion channel activity.
Ref 531079J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Ref 531220J Med Chem. 2010 Nov 11;53(21):7564-72.Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors.
Ref 531563A double-blind, randomized, placebo-controlled, active reference study of Lu AA21004 in patients with major depressive disorder. Int J Neuropsychopharmacol. 2012 Jun;15(5):589-600.
Ref 5317832011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
Ref 532217Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats. Pharmacol Biochem Behav. 2013 Apr;105:41-50.
Ref 532361Monoamine transporter occupancy of a novel triple reuptake inhibitor in baboons and humans using positron emission tomography. J Pharmacol Exp Ther. 2013 Aug;346(2):311-7.
Ref 532463Effect of DA-8031, a novel oral compound for premature ejaculation, on male rat sexual behavior. Int J Urol. 2014 Mar;21(3):325-9.
Ref 5326512013 FDA drug approvals. Nat Rev Drug Discov. 2014 Feb;13(2):85-9.
Ref 532713Antitussives and substance abuse. Subst Abuse Rehabil. 2013 Nov 6;4:75-82.
Ref 533083Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor. Int J Neuropsychopharmacol. 2014 Dec 13;18(2). pii: pyu027.
Ref 533235Dasotraline for the Treatment of Attention-Deficit/Hyperactivity Disorder: A Randomized, Double-Blind, Placebo-Controlled, Proof-of-Concept Trial in Adults. Neuropsychopharmacology. 2015 Nov;40(12):2745-52.
Ref 533382J Med Chem. 1988 Dec;31(12):2247-56.Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity.
Ref 533519J Med Chem. 1983 Jul;26(7):935-47.Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans.
Ref 533558J Med Chem. 1984 Nov;27(11):1508-15.Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins.
Ref 534240J Med Chem. 1996 Oct 11;39(21):4139-41.3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter.
Ref 534352J Med Chem. 1997 Mar 28;40(7):1049-62.Structure-activity studies for a novel series of N-(arylethyl)-N-(1,2,3,4-tetrahydronaphthalen-1-ylmethyl)-N-methylamine s possessing dual 5-HT uptake inhibitingand alpha2-antagonistic activities.
Ref 536103Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418.
Ref 536130Phentermine and anaesthesia. Anaesth Intensive Care. 2005 Aug;33(4):525-7.
Ref 536286Serotonin reuptake inhibitors: the corner stone in treatment of depression for half a century--a medicinal chemistry survey. Curr Top Med Chem. 2006;6(17):1801-23.
Ref 536303Methadone: from pharmacokinetic profile to clinical pharmacology. Encephale. 2006 Jul-Aug;32(4 Pt 1):478-86.
Ref 536306Emerging treatments for depression. Expert Opin Pharmacother. 2006 Dec;7(17):2323-39.
Ref 536331Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28.
Ref 536335Serotonergic drugs : effects on appetite expression and use for the treatment of obesity. Drugs. 2007;67(1):27-55.
Ref 536499Emerging drugs for attention-deficit/hyperactivity disorder. Expert Opin Emerg Drugs. 2007 Sep;12(3):423-34.
Ref 536503Psychopharmacological treatment of dermatological patients--when simply talking does not help. J Dtsch Dermatol Ges. 2007 Dec;5(12):1101-6. Epub 2007 Sep 17.
Ref 536580Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
Ref 536774Treatment of comorbid pain with serotonin norepinephrine reuptake inhibitors. CNS Spectr. 2008 Jul;13(7 Suppl 11):22-6.
Ref 537225Efficacy of treatments for patients with obsessive-compulsive disorder: a systematic review. J Am Acad Nurse Pract. 2009 Apr;21(4):207-13.
Ref 537241Differential involvement of the norepinephrine, serotonin and dopamine reuptake transporter proteins in cocaine-induced taste aversion. Pharmacol Biochem Behav. 2009 Jul;93(1):75-81. Epub 2009 Apr 17.
Ref 537422Clinically relevant drug interactions with new generation antidepressants and antipsychotics. Ther Umsch. 2009 Jun;66(6):485-92.
Ref 537457Augmentation effect of combination therapy of aripiprazole and antidepressants on forced swimming test in mice. Psychopharmacology (Berl). 2009 Jun 11.
Ref 537531Duloxetine for the treatment of generalized anxiety disorder: a review. Neuropsychiatr Dis Treat. 2009;5:23-31. Epub 2009 Apr 8.
Ref 537557Antidepressants and sleep: a review. Perspect Psychiatr Care. 2009 Jul;45(3):191-7.
Ref 537565Changes of functional MRI findings in a patient whose pathological gambling improved with fluvoxamine. Yonsei Med J. 2009 Jun 30;50(3):441-4. Epub 2009 Jun 24.
Ref 537730Placebo controlled double-blind trial of fluvoxamine maleate in the obese. J Psychosom Res. 1986;30(2):143-6.
Ref 537983A non-selective (amitriptyline), but not a selective (citalopram), serotonin reuptake inhibitor is effective in the prophylactic treatment of chronic tension-type headache. J Neurol Neurosurg Psychiatry. 1996 Sep;61(3):285-90.
Ref 543976(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. (Target id: 928).
Ref 548778Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028715)
Ref 549028Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031598)
Ref 549794Clinical pipeline report, company report or official report of Clera Inc.
Ref 550007Clinical pipeline report, company report or official report of Neurosearch.
Ref 550360NSD-644: Phase I started.NeuroSearch A/S (CSE:NEUR), Ballerup, Denmark, GlaxoSmithKline plc (LSE:GSK; GSK), London, U.K.
Ref 551041Clinical pipeline report, company report or official report of Intra-Cellular Therapies, Inc.
Ref 551380Differential behavioural and neurochemical effects of para-methoxyamphetamine and 3,4-methylenedioxymethamphetamine in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2000 Aug;24(6):955-77.
Ref 551382The origin of <span class="caps">MDMA</span> (ecstasy) revisited: the true story reconstructed from the original documents. Addiction. 2006 Sep;101(9):1241-5.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 551828Encyclopedia of Psychopharmacology. Ian Stolerman. 2010. Page(105).
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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