Target Validation Information
TTD ID T27812
Target Name Serotonin transporter (SERT)
Type of Target
Successful
Drug Potency against Target Drug Info IC50 = 2700 nM [65]
Amfepramone Drug Info IC50 = 311000 nM [63]
Amitriptyline Drug Info IC50 = 39 nM [74]
Bupropion Drug Info Ki = 22000 nM [71]
Citalopram Drug Info IC50 = 1.8 nM [74]
Clomipramine Drug Info IC50 = 1.5 nM [74]
Cocaine Drug Info IC50 = 480 nM [73]
Dexfenfluramine Drug Info pKi = 5.41 [68]
Escitalopram Drug Info IC50 = 1.5 nM [69]
Fluoxetine Drug Info IC50 = 6.8 nM [74]
Fluvoxamine Drug Info IC50 = 3.8 nM [74]
Paroxetine Drug Info IC50 = 0.29 nM [74]
Sertraline Drug Info IC50 = 0.19 nM [74]
Sibutramine Drug Info IC50 = 477000 nM [62]
Tianeptine Drug Info IC50 = 11320 nM
Trazodone Drug Info IC50 = 0.58 mM [70]
Venlafaxine Drug Info IC50 = 210 nM
Drug Info Ki = 12 nM [67]
Bicifadine Drug Info IC50 = 120 nM [28]
DOV-216303 Drug Info Ki = 13.8 nM [7]
OPC-14523 Drug Info IC50 = 80 nM [64]
R-sibutramine metabolite Drug Info Ki = 5100 nM [72]
Vilazodone Drug Info IC50 = 0.5 nM [61]
YM-992 Drug Info Ki = 21 nM [61]
Drug Info IC50 = 27 nM [28]
Drug Info IC50 = 2000 nM [59]
Drug Info IC50 = 27 nM [28]
Drug Info IC50 = 2000 nM [59]
((3R,4R)-4-(o-tolyloxy)chroman-3-yl)methanamine Drug Info IC50 = 3800 nM [32]
(+/-)-3-((naphthalen-2-yloxy)methyl)pyrrolidine Drug Info IC50 = 25 nM [40]
(+/-)-nantenine Drug Info Ki = 244 nM [49]
(2R,3R)-iodoreboxetine Drug Info Ki = 646 nM [33]
(2R,3R)-iodoreboxetine Drug Info Ki = 646 nM [33]
(2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 51.5 nM [42]
(2R,3S)-2-[(2-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 51.5 nM [42]
(2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 154 nM [42]
(2R,3S)-2-[(3-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 154 nM [42]
(2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 34.5 nM [42]
(2R,3S)-2-[(4-Iodophenoxy)phenylmethyl]morpholine Drug Info Ki = 34.5 nM [42]
(2S,3S)-iodoreboxetine Drug Info Ki = 2793 nM [33]
(2S,3S)-iodoreboxetine Drug Info Ki = 2793 nM [33]
(cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 240 nM [28]
(cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 240 nM [28]
(R)-2-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info Ki = 8 nM [53]
(R)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 20 nM [40]
(R)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 42 nM [40]
(R)-DULOXETINE Drug Info Ki = 8.8 nM [37]
(R)-DULOXETINE Drug Info Ki = 8.8 nM [37]
(R)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 5 nM [44]
(R)-N-isopropyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 15 nM [44]
(R)-Norfluoxetine Drug Info IC50 = 13 nM [36]
(S)-3-(naphthalen-2-ylmethoxy)pyrrolidine Drug Info IC50 = 23 nM [40]
(S)-6-(pyrrolidin-3-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 37 nM [40]
(S)-N-isobutyl-N-(pyrrolidin-3-yl)-2-naphthamide Drug Info IC50 = 3 nM [44]
(S)-NORDULOXETINE Drug Info IC50 = 25.6 nM [45]
(S)-Norfluoxetine Drug Info IC50 = 46 nM [36]
1-(1,2-diphenylethyl)piperazine Drug Info IC50 = 14 nM [13]
1-(1,3-diphenylpropyl)piperazine Drug Info IC50 = 23 nM [14]
1-(1,4-diphenylbutan-2-yl)piperazine Drug Info IC50 = 23 nM [14]
1-(1-(2-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 24 nM [53]
1-(1-(4-FLUOROPHENYL)-2-(2-(TRIFLUOROMETHOXY)PHENYL)ETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 24 nM [53]
1-(1-phenyl-2-(2-propoxyphenyl)ethyl)piperazine Drug Info Ki = 18 nM [53]
1-(1-phenyl-2-(pyridin-2-yl)ethyl)piperazine Drug Info IC50 = 230 nM [14]
1-(1-phenyl-2-(pyridin-4-yl)ethyl)piperazine Drug Info IC50 = 38 nM [14]
1-(1-phenyl-2-o-tolylethyl)piperazine Drug Info IC50 = 12 nM [13]
1-(2-((3-fluorophenoxy)methyl)phenyl)piperazine Drug Info Ki = 17 nM [47]
1-(2-(2-(DIFLUOROMETHOXY)PHENYL)-1-PHENYLETHYL)PIPERAZINE (ENANTIOMERIC MIX) Drug Info Ki = 27 nM [53]
1-(2-(2-bromophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 15 nM [13]
1-(2-(2-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 5.4 nM [13]
1-(2-(2-ethoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 13 nM [13]
1-(2-(2-ethylphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 16 nM [13]
1-(2-(2-fluorobenzyloxy)phenyl)piperazine Drug Info Ki = 978 nM [47]
1-(2-(2-methoxyphenyl)-1-phenylethyl)piperazine Drug Info Ki = 4 nM [53]
1-(2-(3-chlorophenyl)-1-phenylethyl)piperazine Drug Info IC50 = 9.4 nM [13]
1-(2-(3-fluorophenoxy)phenyl)piperazine Drug Info Ki = 3100 nM [47]
1-(2-(3-methoxyphenyl)-1-phenylethyl)piperazine Drug Info IC50 = 25 nM [13]
1-(2-(4-fluorophenoxy)phenyl)piperazine Drug Info Ki = 994 nM [47]
1-(2-(6-fluoronaphthalen-2-yl)ethyl)piperazine Drug Info IC50 = 11 nM [40]
1-(2-(benzyloxy)phenyl)piperazine Drug Info Ki = 1140 nM [47]
1-(2-(naphthalen-1-yl)-1-phenylethyl)piperazine Drug Info IC50 = 12 nM [14]
1-(2-(naphthalen-2-yl)-1-phenylethyl)piperazine Drug Info IC50 = 17 nM [14]
1-(2-(naphthalen-2-yl)ethyl)piperazine Drug Info IC50 = 88 nM [40]
1-(2-(phenoxymethyl)phenyl)piperazine Drug Info Ki = 780 nM [47]
1-(2-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 2020 nM [11]
1-(2-phenoxyphenyl)piperazine Drug Info Ki = 1880 nM [47]
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol Drug Info Ki = 0.7 nM [6]
1-(3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol Drug Info Ki = 0.7 nM [6]
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol Drug Info Ki = 3 nM [6]
1-(3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol Drug Info Ki = 3 nM [6]
1-(3-chlorophenyl)-2-(piperidin-1-yl)propan-1-one Drug Info Ki = 5479 nM [46]
1-(3-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 1070 nM [11]
1-(3-methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 4400 nM [11]
1-(4-Benzylsulfanyl-phenyl)-propylamine Drug Info IC50 = 679 nM [43]
1-(4-Benzylsulfanyl-phenyl)-propylamine Drug Info IC50 = 679 nM [43]
1-(4-bromophenyl)-2-(tert-butylamino)propan-1-one Drug Info IC50 = 4508 nM [52]
1-(4-bromophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 1050 nM [11]
1-(4-iodophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 197 nM [11]
1-(4-nitrophenyl)-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 1110 nM [11]
1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 140 nM [28]
1-(benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 140 nM [28]
1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 50 nM [28]
1-(naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 50 nM [28]
1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 4500 nM [28]
1-(thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 4500 nM [28]
1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 160 nM [28]
1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 160 nM [28]
1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 2900 nM [28]
1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 2900 nM [28]
1-Methyl-2-(4-phenylsulfanyl-phenyl)-ethylamine Drug Info IC50 = 14330 nM [43]
1-Methyl-2-(4-phenylsulfanyl-phenyl)-ethylamine Drug Info IC50 = 14330 nM [43]
1-Methyl-4-p-tolyl-piperidine-4-carbonitrile Drug Info Ki = 13700 nM [1]
1-Methyl-4-p-tolyl-piperidine-4-carbonitrile Drug Info Ki = 13700 nM [1]
1-naphthalen-2-yl-2-pyrrolidin-1-yl-pentan-1-one Drug Info IC50 = 46 nM [11]
1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 5200 nM [28]
1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 5200 nM [28]
10R-hydroxylobel-7-ene Drug Info Ki = 7500 nM [15]
10R-hydroxylobel-7-ene Drug Info Ki = 7500 nM [15]
10R-hydroxylobelane Drug Info Ki = 7300 nM [15]
10R-hydroxylobelane Drug Info Ki = 7300 nM [15]
10S-hydroxylobel-7-ene Drug Info Ki = 19000 nM [15]
10S-hydroxylobel-7-ene Drug Info Ki = 19000 nM [15]
10S-hydroxylobelane Drug Info Ki = 4270 nM [15]
10S-hydroxylobelane Drug Info Ki = 4270 nM [15]
1S,2R-milnacipran Drug Info IC50 = 28 nM [35]
1S,2R-milnacipran Drug Info IC50 = 28 nM [35]
2-(2'-Aminoethyl)-5-benzyltetrahydrofuran Drug Info IC50 = 2260 nM [39]
2-(2-chlorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 57 nM [50]
2-(2-fluorophenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 728 nM [50]
2-(2-methoxyphenoxy)-3-(piperidin-4-yl)pyridine Drug Info Ki = 610 nM [50]
2-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 87 nM [13]
2-(3-Methyl-piperazin-1-yl)-6-nitro-quinoline Drug Info Ki = 22.19 nM [2]
2-(3-Methyl-piperazin-1-yl)-6-nitro-quinoline Drug Info Ki = 22.19 nM [2]
2-(Aminomethyl)-5-(1'-naphthethyl)tetrahydrofuran Drug Info IC50 = 23 nM [39]
2-(Aminomethyl)-5-(1'-naphthyl)tetrahydrofuran Drug Info IC50 = 24 nM [39]
2-(Aminomethyl)-5-(2'-naphthyl)tetrahydrofuran Drug Info IC50 = 4 nM [39]
2-(Aminomethyl)-5-phenethyltetrahydrofuran Drug Info IC50 = 129 nM [39]
2-(N-Cyclopentylamino)-3'-methoxypropiophenone Drug Info IC50 = 6900 nM [52]
2-(N-Cyclopropylamino)-3-chloropropiophenone Drug Info Ki = 3420 nM [46]
2-(N-tert-Butylamino)-3',4'-dichloropropiophenone Drug Info Ki = 1480 nM [46]
2-(tert-butylamino)-1-(3-chlorophenyl)butan-1-one Drug Info IC50 = 16000 nM [52]
2-(tert-Butylamino)-3',4'-dichlorobutyrophenone Drug Info IC50 = 790 nM [46]
2-(tert-Butylamino)-3',4'-dichloropentanophenone Drug Info Ki = 842 nM [46]
2-Amino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1290 nM [43]
2-Amino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1290 nM [43]
2-Amino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 1403 nM [43]
2-Amino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 1403 nM [43]
2-Amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 611 nM [43]
2-Amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 611 nM [43]
2-Amino-1-(4-methylthiophenyl)propane Drug Info IC50 = 74 nM [43]
2-Amino-1-(4-methylthiophenyl)propane Drug Info IC50 = 74 nM [43]
2-Aminomethyl-5-(p-bromophenyl)tetrahydrofuran Drug Info IC50 = 50 nM [39]
2-Aminomethyl-5-(p-chlorophenyl)tetrahydrofuran Drug Info IC50 = 32 nM [39]
2-Aminomethyl-5-(p-methoxyphenyl)tetrahydrofuran Drug Info IC50 = 617 nM [39]
2-Aminomethyl-5-(p-t-butylphenyl)tetrahydrofuran Drug Info IC50 = 636 nM [39]
2-Aminomethyl-5-(phenyl)tetrahydrofuran Drug Info IC50 = 1714 nM [39]
2-N,N-Dimethylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 520 nM [43]
2-N,N-Dimethylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 520 nM [43]
2-N-(Isopropyl)amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 1939 nM [43]
2-N-(Isopropyl)amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 1939 nM [43]
2-N-(n-Propyl)amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 621 nM [43]
2-N-(n-Propyl)amino-1-(4-methylthiophenyl)butane Drug Info IC50 = 621 nM [43]
2-N-Allylamino-1-(4-methylthiophenyl)propan Drug Info IC50 = 524 nM [43]
2-N-Allylamino-1-(4-methylthiophenyl)propan Drug Info IC50 = 524 nM [43]
2-N-Cyclopropylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 872 nM [43]
2-N-Cyclopropylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 872 nM [43]
2-N-Ethylamino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1804 nM [43]
2-N-Ethylamino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1804 nM [43]
2-N-Ethylamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 478 nM [43]
2-N-Ethylamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 478 nM [43]
2-N-Ethylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 823 nM [43]
2-N-Ethylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 823 nM [43]
2-N-Ethylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 963 nM [43]
2-N-Ethylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 963 nM [43]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1446 nM [43]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)butane Drug Info IC50 = 1446 nM [43]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 625 nM [43]
2-N-Hydroxyamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 625 nM [43]
2-N-Hydroxyamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 598 nM [43]
2-N-Hydroxyamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 598 nM [43]
2-N-Hydroxyamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 436 nM [43]
2-N-Hydroxyamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 436 nM [43]
2-N-Methoxyamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 664 nM [43]
2-N-Methoxyamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 664 nM [43]
2-N-Methylamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 724 nM [43]
2-N-Methylamino-1-(4-ethylthiophenyl)propane Drug Info IC50 = 724 nM [43]
2-N-Methylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 437 nM [43]
2-N-Methylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 437 nM [43]
2-N-Methylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 417 nM [43]
2-N-Methylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 417 nM [43]
2-N-Propargylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 399 nM [43]
2-N-Propargylamino-1-(4-methylthiophenyl)butane Drug Info IC50 = 399 nM [43]
2-N-Propargylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 688 nM [43]
2-N-Propargylamino-1-(4-methylthiophenyl)propane Drug Info IC50 = 688 nM [43]
2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole Drug Info IC50 = 887 nM [60]
2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole Drug Info IC50 = 887 nM [60]
2-phenoxy-3-(piperidin-4-yl)pyridine Drug Info Ki = 1890 nM [50]
2-[1,4]Diazepan-1-yl-6-nitro-quinoline Drug Info Ki = 1.9 nM [2]
2-[1,4]Diazepan-1-yl-6-nitro-quinoline Drug Info Ki = 1.9 nM [2]
3-(1H-indol-1-yl)-N-methyl-3-phenylpropan-1-amine Drug Info IC50 = 327 nM [34]
3-(1H-indol-3-yl)-N,N-dimethylpropan-1-amine Drug Info IC50 = 58 nM [22]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzamide Drug Info IC50 = 210 nM [13]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)benzonitrile Drug Info IC50 = 4 nM [13]
3-(2-phenyl-2-(piperazin-1-yl)ethyl)phenol Drug Info IC50 = 9.5 nM [13]
3-(3,4-dichlorophenyl)-2-nortropene Drug Info Ki = 0.3 nM [48]
3-(3,4-dichlorophenyl)-2-nortropene Drug Info Ki = 0.3 nM [48]
3-(3-aminocyclopentyl)-1H-indole-5-carbonitrile Drug Info IC50 = 32 nM [55]
3-(4-Chlorophenyl)-2-nortropene Drug Info Ki = 2.8 nM [48]
3-(4-Chlorophenyl)-2-nortropene Drug Info Ki = 2.8 nM [48]
3-(4-Fluorophenyl)-2-nortropene Drug Info Ki = 129 nM [48]
3-(4-Fluorophenyl)-2-nortropene Drug Info Ki = 129 nM [48]
3-(4-Trifluoromethylphenyl)-2-nortropene Drug Info Ki = 1.8 nM [48]
3-(4-Trifluoromethylphenyl)-2-nortropene Drug Info Ki = 1.8 nM [48]
3-(piperidin-4-yl)-2-(o-tolyloxy)pyridine Drug Info Ki = 292 nM [50]
3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane Drug Info Ki = 247 nM [48]
3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane Drug Info Ki = 247 nM [48]
3-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 12.62 nM [2]
3-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 12.62 nM [2]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 46 nM [3]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 46 nM [3]
3-Phenyl-2-nortropene Drug Info Ki = 176 nM [48]
3-Phenyl-2-nortropene Drug Info Ki = 176 nM [48]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info Ki = 1640 nM [16]
3alpha-(bis-chloro-phenylmethoxy)tropane Drug Info Ki = 1640 nM [16]
4-((naphthalen-2-yloxy)methyl)piperidine Drug Info IC50 = 8 nM [40]
4-(1H-indol-3-yl)-N,N-dimethylcyclohex-3-enamine Drug Info IC50 = 3.1 nM [18]
4-(2-((3-fluorophenoxy)methyl)phenyl)piperidine Drug Info Ki = 49 nM [47]
4-(2-((dimethylamino)methyl)phenoxy)benzonitrile Drug Info IC50 = 60 nM [30]
4-(2-(2-fluoro-5-methylphenoxy)phenyl)piperidine Drug Info Ki = 26 nM [47]
4-(2-(2-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 56 nM [47]
4-(2-(3-chlorophenoxy)phenyl)piperidine Drug Info Ki = 211 nM [47]
4-(2-(3-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 2 nM [47]
4-(2-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 901 nM [47]
4-(2-(4-fluorobenzyloxy)phenyl)piperidine Drug Info Ki = 274 nM [47]
4-(2-(4-fluorophenoxy)-4-methylphenyl)piperidine Drug Info Ki = 427 nM [47]
4-(2-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 319 nM [47]
4-(2-(benzyloxy)-3-fluorophenyl)piperidine Drug Info Ki = 2970 nM [47]
4-(2-(benzyloxy)-6-fluorophenyl)piperidine Drug Info Ki = 28 nM [47]
4-(2-(benzyloxy)phenyl)piperidine Drug Info Ki = 74 nM [47]
4-(2-(phenoxymethyl)phenyl)piperidine Drug Info Ki = 364 nM [47]
4-(2-fluoro-6-(2-fluorophenoxy)phenyl)piperidine Drug Info Ki = 1260 nM [50]
4-(2-fluoro-6-(3-fluorophenoxy)phenyl)piperidine Drug Info Ki = 1040 nM [47]
4-(2-fluoro-6-(4-fluorophenoxy)phenyl)piperidine Drug Info Ki = 157 nM [47]
4-(2-fluoro-6-phenoxyphenyl)piperidine Drug Info Ki = 706 nM [47]
4-(2-phenoxyphenyl)piperidine Drug Info Ki = 1760 nM [47]
4-(3-fluoro-2-phenoxyphenyl)piperidine Drug Info Ki = 2330 nM [47]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [54]
4-Allyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.67 nM [4]
4-Allyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.67 nM [4]
4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 126.86 nM [4]
4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 126.86 nM [4]
4-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 0.37 nM [4]
4-Bromo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 0.37 nM [4]
4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 5.23 nM [4]
4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 5.23 nM [4]
4-Iodo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.73 nM [4]
4-Iodo-6-nitro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.73 nM [4]
6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 1800 nM [28]
6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane Drug Info IC50 = 1800 nM [28]
6,8-Dinitro-2-piperazin-1-yl-quinoline Drug Info Ki = 312.85 nM [2]
6,8-Dinitro-2-piperazin-1-yl-quinoline Drug Info Ki = 312.85 nM [2]
6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline Drug Info IC50 = 640 nM [28]
6-(3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline Drug Info IC50 = 640 nM [28]
6-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 15 nM [40]
6-Bromo-2-piperazin-1-yl-quinoline Drug Info Ki = 0.91 nM [2]
6-Bromo-2-piperazin-1-yl-quinoline Drug Info Ki = 0.91 nM [2]
6-Chloro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.68 nM [2]
6-Chloro-2-piperazin-1-yl-quinoline Drug Info Ki = 1.68 nM [2]
6-Iodo-2-piperazin-1-yl-quinoline Drug Info Ki = 6.6 nM [2]
6-Iodo-2-piperazin-1-yl-quinoline Drug Info Ki = 6.6 nM [2]
6-Nitro-2-piperazin-1-yl-4-vinyl-quinoline Drug Info Ki = 1.82 nM [4]
6-Nitro-2-piperazin-1-yl-4-vinyl-quinoline Drug Info Ki = 1.82 nM [4]
6-Nitro-4-phenyl-2-piperazin-1-yl-quinoline Drug Info Ki = 60.03 nM [4]
6-Nitro-4-phenyl-2-piperazin-1-yl-quinoline Drug Info Ki = 60.03 nM [4]
6-nitroquipazine Drug Info Ki = 0.24 nM [17]
6-nitroquipazine Drug Info Ki = 0.24 nM [17]
7-(piperidin-4-ylmethoxy)-2-naphthonitrile Drug Info IC50 = 3 nM [40]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 390 nM [3]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane Drug Info Ki = 390 nM [3]
8R-hydroxylobel-9-ene Drug Info Ki = 860 nM [51]
8R-hydroxylobel-9-ene Drug Info Ki = 860 nM [51]
8R-hydroxylobelane Drug Info Ki = 150 nM [15]
8R-hydroxylobelane Drug Info Ki = 150 nM [15]
8S-hydroxylobel-9-ene Drug Info Ki = 3750 nM [15]
8S-hydroxylobel-9-ene Drug Info Ki = 3750 nM [15]
8S-hydroxylobelane Drug Info Ki = 2220 nM [15]
8S-hydroxylobelane Drug Info Ki = 2220 nM [15]
A-80426 Drug Info IC50 = 13.1 nM [60]
A-80426 Drug Info IC50 = 13.1 nM [60]
Beta-methoxyamphetamine Drug Info IC50 = 173 nM [43]
Beta-methoxyamphetamine Drug Info IC50 = 173 nM [43]
Biphenyl-2-ylmethyl-(S)-pyrrolidin-3-yl-amine Drug Info Ki = 1070 nM [31]
COCAINE.HCL Drug Info Ki = 306 nM [20]
COCAINE.HCL Drug Info Ki = 306 nM [20]
Cyclohexyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info IC50 = 8000 nM [5]
Cyclohexyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info IC50 = 8000 nM [5]
Cyclopentyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info IC50 = 10000 nM [5]
Cyclopentyl-(3,4-dichloro-phenyl)-acetonitrile Drug Info IC50 = 10000 nM [5]
D-166A Drug Info Ki = 11216 nM [27]
D-166A Drug Info Ki = 11216 nM [27]
D-211A Drug Info Ki = 11884 nM [27]
D-211A Drug Info Ki = 11884 nM [27]
D-211B Drug Info Ki = 1484 nM [27]
D-211B Drug Info Ki = 1484 nM [27]
D-254C Drug Info Ki = 1391 nM [27]
D-254C Drug Info Ki = 1391 nM [27]
D-257A Drug Info Ki = 12904 nM [27]
D-257A Drug Info Ki = 12904 nM [27]
D-257C Drug Info Ki = 7414 nM [27]
D-257C Drug Info Ki = 7414 nM [27]
Difluorobenztropine Drug Info Ki = 3260 nM [16]
Difluorobenztropine Drug Info Ki = 3260 nM [16]
Erythro-3,4-dichloromethylphenidate hydrochloride Drug Info Ki = 2570 nM [20]
Erythro-3,4-dichloromethylphenidate hydrochloride Drug Info Ki = 2570 nM [20]
Irindalone Drug Info IC50 = 14000 nM [56]
Irindalone Drug Info IC50 = 14000 nM [56]
Isobutyl-(4-methyl-benzyl)-piperidin-4-yl-amine Drug Info Ki = 0.99 nM [12]
JNJ-28583867 Drug Info Ki = 3.7 nM [24]
KF-A5 Drug Info IC50 = 7800 nM [23]
KF-A6 Drug Info IC50 = 3500 nM [23]
LITOXETINE Drug Info IC50 = 5.9 nM [44]
MDL-28618 Drug Info IC50 = 190 nM [32]
METHYLENEDIOXYAMPHETAMINE Drug Info IC50 = 478 nM [43]
METHYLENEDIOXYAMPHETAMINE Drug Info IC50 = 478 nM [43]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info IC50 = 1060 nM [43]
METHYLENEDIOXYMETHAMPHETAMINE Drug Info IC50 = 1060 nM [43]
N*1*-(6-Nitro-quinolin-2-yl)-ethane-1,2-diamine Drug Info Ki = 164.3 nM [2]
N*1*-(6-Nitro-quinolin-2-yl)-ethane-1,2-diamine Drug Info Ki = 164.3 nM [2]
N,N-dimethyl(2-phenoxyphenyl)methanamine Drug Info IC50 = 660 nM [26]
N-(2-oxazolemethyl)milnacipran Drug Info IC50 = 1600 nM [25]
N-(piperidin-4-yl)-N-propyl-2-naphthamide Drug Info IC50 = 28.3 nM [44]
N-benzyl-N-isobutylpiperidin-4-amine Drug Info Ki = 8.4 nM [12]
N-cyclobutyl-N-(piperidin-4-yl)-2-naphthamide Drug Info IC50 = 10 nM [44]
NISOXETINE Drug Info Ki = 277 nM [37]
NISOXETINE Drug Info Ki = 277 nM [37]
O-DESMETHYL TRAMADOL Drug Info IC50 = 4600 nM [10]
Para-chloroamphetamine Drug Info IC50 = 182 nM [43]
Para-chloroamphetamine Drug Info IC50 = 182 nM [43]
PF-18298 Drug Info Ki = 6 nM [53]
PF-3409409 Drug Info Ki = 224 nM [41]
PF-526014 Drug Info Ki = 10 nM [53]
PYROVALERONE Drug Info IC50 = 2780 nM [11]
QUIPAZINE Drug Info Ki = 63 nM [2]
QUIPAZINE Drug Info Ki = 63 nM [2]
R-226161 Drug Info Ki = 1.2 nM [19]
R-NORDULOXETINE Drug Info IC50 = 6.8 nM [45]
Reboxetine Drug Info Ki = 661 nM [38]
RTI-219 Drug Info IC50 = 2710 nM [21]
S-34324 Drug Info Ki = 77 nM [9]
TEFLUDAZINE Drug Info IC50 = 7000 nM [57]
TEFLUDAZINE Drug Info IC50 = 7000 nM [57]
Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride Drug Info Ki = 5140 nM [20]
Threo-1-aza-5-phenyl[4.4.0]decane hydrochloride Drug Info Ki = 5140 nM [20]
Threo-3,4-dichlororitalinol hydrochloride Drug Info Ki = 276 nM [20]
Threo-3,4-dichlororitalinol hydrochloride Drug Info Ki = 276 nM [20]
Trans-3-(o-tolyloxy)-2,3-dihydro-1H-inden-1-amine Drug Info IC50 = 10000 nM [29]
WIN-35065 Drug Info Ki = 1900 nM [21]
WIN-35065 Drug Info Ki = 1900 nM [21]
WIN-35066-2 Drug Info Ki = 178 nM [8]
ZIMELIDINE Drug Info IC50 = 4500 nM [58]
ZIMELIDINE Drug Info IC50 = 4500 nM [58]
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine Drug Info Ki = 3 nM [6]
[3-(3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine Drug Info Ki = 3 nM [6]
[3H]WIN35428 Drug Info IC50 = 5060 nM [59]
[3H]WIN35428 Drug Info IC50 = 5060 nM [59]
Action against Disease Model Vilazodone Drug Info EMD 68843 (vilazodone) is a novel compound with combined high affinity and selectivity for the 5-hydroxytryptamine (5-HT) transporter and 5-HT(1A) receptors. In Sf9 cells, EMD 68843 increased guanosine 5'-O-(3-[(35)S]thiotriphosphate) binding to 69% of the magnitude of the full 5-HT(1A) receptor agonist R-(1)-trans-8-hydroxy-2-[N-n-propyl-N-(39-iodo-29-propenyl)] aminotetralin (8-OH-PIPAT), indicating that it is a partial agonist at 5-HT(1A) receptors. Acute, systemic administration of EMD 68843 produced a larger maximal increase of extracellular 5-HT than the SSRI fluoxetine in both the ventral hippocampus (HPv) (558 versus 274%) and the frontal cortex (FC) (527 versus 165%). Regional differences in the response to the two drugs were also observed. These effects maybe attributed to the differential regulation of 5-HT release in the HPv and FC by 5-HT(1A) autoreceptors. When challenged with the 5-HT(1A) receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), EMD 68843-induced increases in extracellular 5-HT were greatly reduced in the HPv but to a lesser extent in the FC. In behavioral studies, EMD 68843 produced antidepressant-like effects in the forced swimming test in both rats and mice but only within a narrow dosage range. Like fluoxetine, [66]
References
REF 1 Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine. Bioorg Med Chem Lett. 1999 Dec 6;9(23):3273-6.
REF 2 Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1. Bioorg Med Chem Lett. 2000 Jul 17;10(14):1559-62.
REF 3 3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter. Bioorg Med Chem Lett. 2000 Nov 6;10(21):2445-7.
REF 4 Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 2: 4-substituted 6-nitroquipazines. Bioorg Med Chem Lett. 2002 Mar 11;12(5):811-5.
REF 5 Synthesis and evaluation of dopamine and serotonin transporter inhibition by oxacyclic and carbacyclic analogues of methylphenidate. J Med Chem. 2003 Apr 10;46(8):1538-45.
REF 6 Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters. J Med Chem. 2004 May 6;47(10):2624-34.
REF 7 DOV 216,303, a "triple" reuptake inhibitor: safety, tolerability, and pharmacokinetic profile. J Clin Pharmacol. 2004 Dec;44(12):1360-7.
REF 8 Monoamine transporter binding, locomotor activity, and drug discrimination properties of 3-(4-substituted-phenyl)tropane-2-carboxylic acid methyl e... J Med Chem. 2004 Dec 2;47(25):6401-9.
REF 9 Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking... J Med Chem. 2005 Mar 24;48(6):2054-71.
REF 10 Derivatives of tramadol for increased duration of effect. Bioorg Med Chem Lett. 2006 Feb;16(3):691-4.
REF 11 1-(4-Methylphenyl)-2-pyrrolidin-1-yl-pentan-1-one (Pyrovalerone) analogues: a promising class of monoamine uptake inhibitors. J Med Chem. 2006 Feb 23;49(4):1420-32.
REF 12 N-Alkyl-N-arylmethylpiperidin-4-amines: novel dual inhibitors of serotonin and norepinephrine reuptake. Bioorg Med Chem Lett. 2006 May 15;16(10):2714-8.
REF 13 N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4345-8.
REF 14 Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4349-53.
REF 15 Des-keto lobeline analogs with increased potency and selectivity at dopamine and serotonin transporters. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5018-21.
REF 16 Structure-activity relationship studies on a novel series of (S)-2beta-substituted 3alpha-[bis(4-fluoro- or 4-chlorophenyl)methoxy]tropane analogue... J Med Chem. 2006 Oct 19;49(21):6391-9.
REF 17 Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 5: 2'-Substituted 6-nitroquipazines. Bioorg Med Chem. 2007 May 15;15(10):3499-504.
REF 18 Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3099-104.
REF 19 Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-a... Bioorg Med Chem. 2007 Jun 1;15(11):3649-60.
REF 20 Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate. J Med Chem. 2007 May 31;50(11):2718-31.
REF 21 Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-... J Med Chem. 2007 Jul 26;50(15):3686-95.
REF 22 Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5647-51.
REF 23 Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. Antimicrob Agents Chemother. 2007 Nov;51(11):4133-40.
REF 24 Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors. Bioorg Med Chem Lett. 2008 Jan 1;18(1):39-43.
REF 25 Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1346-9.
REF 26 1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity. Bioorg Med Chem Lett. 2008 Jan 15;18(2):596-9.
REF 27 Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an ex... Bioorg Med Chem. 2008 Mar 15;16(6):2769-78.
REF 28 Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3682-6.
REF 29 Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI). Bioorg Med Chem Lett. 2008 Jul 15;18(14):4224-7.
REF 30 Designing rapid onset selective serotonin re-uptake inhibitors. 2: structure-activity relationships of substituted (aryl)benzylamines. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4018-21.
REF 31 Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modu... Bioorg Med Chem Lett. 2008 Aug 1;18(15):4355-9.
REF 32 Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint. Bioorg Med Chem Lett. 2008 Aug 15;18(16):4495-8.
REF 33 New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4940-3.
REF 34 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. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6067-70.
REF 35 Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropath... J Med Chem. 2008 Nov 27;51(22):7265-72.
REF 36 Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Jan 1;17(1):337-43.
REF 37 1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors. Bioorg Med Chem Lett. 2009 Jan 1;19(1):58-61.
REF 38 Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomogra... J Med Chem. 2009 Jan 8;52(1):62-73.
REF 39 2,5-Disubstituted tetrahydrofurans as selective serotonin re-uptake inhibitors. Bioorg Med Chem. 2009 Mar 1;17(5):2047-68.
REF 40 Design and optimization of selective serotonin re-uptake inhibitors with high synthetic accessibility. Part 1. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2329-32.
REF 41 Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more po... Bioorg Med Chem Lett. 2009 Aug 15;19(16):4579-83.
REF 42 Design and synthesis of (2R,3S)-iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4996-8.
REF 43 Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents. Eur J Med Chem. 2009 Dec;44(12):4862-88.
REF 44 Bioorg 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 45 Inhibition of serotonin and norepinephrine reuptake and inhibition of phosphodiesterase by multi-target inhibitors as potential agents for depression. Bioorg Med Chem. 2009 Oct 1;17(19):6890-7.
REF 46 Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction. J Med Chem. 2009 Nov 12;52(21):6768-81.
REF 47 Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1... Bioorg Med Chem Lett. 2009 Dec 1;19(23):6604-7.
REF 48 Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6865-8.
REF 49 Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31.
REF 50 Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agon... Bioorg Med Chem Lett. 2010 Feb 1;20(3):1114-7.
REF 51 Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters. Bioorg Med Chem. 2010 Jan 15;18(2):640-9.
REF 52 Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for smoking cessation. J Med Chem. 2010 Mar 11;53(5):2204-14.
REF 53 Second generation N-(1,2-diphenylethyl)piperazines as dual serotonin and noradrenaline reuptake inhibitors: improving metabolic stability and reduc... Bioorg Med Chem Lett. 2010 Jun 15;20(12):3788-92.
REF 54 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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 55 Conformationally restricted homotryptamines. Part 7: 3-cis-(3-aminocyclopentyl)indoles as potent selective serotonin reuptake inhibitors. J Med Chem. 2010 Nov 11;53(21):7564-72.
REF 56 Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity. J Med Chem. 1988 Dec;31(12):2247-56.
REF 57 Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans. J Med Chem. 1983 Jul;26(7):935-47.
REF 58 Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins. J Med Chem. 1984 Nov;27(11):1508-15.
REF 59 3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine trans... J Med Chem. 1996 Oct 11;39(21):4139-41.
REF 60 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 upt... J Med Chem. 1997 Mar 28;40(7):1049-62.
REF 61 Serotonin 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 62 Sibutramine, a serotonin uptake inhibitor, increases dopamine concentrations in rat striatal and hypothalamic extracellular fluid. Neuropharmacology. 2000 Sep;39(12):2352-9.
REF 63 Uptake and release effects of diethylpropion and its metabolites with biogenic amine transporters. Bioorg Med Chem. 2000 Dec;8(12):2689-92.
REF 64 Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001 Dec;41(8):976-88.
REF 65 Block of volume-regulated anion channels by selective serotonin reuptake inhibitors. Naunyn Schmiedebergs Arch Pharmacol. 2002 Aug;366(2):158-65.
REF 66 Behavioral and neurochemical effects of 5-(4-[4-(5-Cyano-3-indolyl)-butyl)-butyl]-1-piperazinyl)-benzofuran-2-carboxamide (EMD 68843): a combined selective inhibitor of serotonin reuptake and 5-hydroxytryptamine(1A) receptor partial agonist. J Pharmacol Exp Ther. 2002 Sep;302(3):1220-7.
REF 67 Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor. Eur J Pharmacol. 2003 Feb 14;461(2-3):99-104.
REF 68 5-HT2C receptor agonists as potential drugs for the treatment of obesity. Curr Top Med Chem. 2003;3(8):885-97.
REF 69 Stereoisomers in Psychiatry: The Case of Escitalopram. Prim Care Companion J Clin Psychiatry. 2002 Feb;4(1):20-24.
REF 70 Synthesis and biological evaluation of 2-(4-fluorophenoxy)-2-phenyl-ethyl piperazines as serotonin-selective reuptake inhibitors with a potentially improved adverse reaction profile. Bioorg Med Chem. 2004 Mar 15;12(6):1483-91.
REF 71 BCL-2 family antagonists for cancer therapy. Nat Rev Drug Discov. 2008 Dec;7(12):989-1000.
REF 72 The contribution of metabolites to the rapid and potent down-regulation of rat cortical beta-adrenoceptors by the putative antidepressant sibutramine hydrochloride. Neuropharmacology. 1989 Feb;28(2):129-34.
REF 73 Novel 2-substituted cocaine analogs: uptake and ligand binding studies at dopamine, serotonin and norepinephrine transport sites in the rat brain. J Pharmacol Exp Ther. 1995 Mar;272(3):1176-86.
REF 74 Selective serotonin reuptake inhibitors in affective disorders--I. Basic pharmacology. J Psychopharmacol. 1998;12(3 Suppl B):S5-20.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.