Therapeutic Targets Database
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TTD Target ID: TTDR01195

Target Information
NameSerotonin transporter    
Type of targetResearch target    
Synonyms5-HTT    
DiseaseDepression
[ICD9: 311   ICD10: F32]
[1]
Target ValidationClick to Find Target Validation Information.    
Inhibitor (2R,3R)-iodoreboxetine[2]
(2R,3S)-2-[[3]
(2R,3S)-2-[[3]
(2R,3S)-2-[[3]
(2S,3S)-iodoreboxetine[2]
(R)-DULOXETINE[4]
(cis)-1,6-diphenyl-3-aza-bicyclo[3.1.0]hexane[5]
1- (3,4-Dichloro-phenyl)-3-diethylamino-indan-5-ol[6]
1- (3,4-Dichloro-phenyl)-3-methylamino-indan-5-ol[6]
1- (3,4-dichlorophenyl)-3-aza-bicyclo[3.1.0]hexane[5]
1- (4-Benzylsulfanyl-phenyl)-propylamine[7]
1- (benzofuran-2-yl)-3-aza-bicyclo[3.1.0]hexane[5]
1- (naphthalen-2-yl)-3-aza-bicyclo[3.1.0]hexane[5]
1- (thiophen-2-yl)-3-aza-bicyclo[3.1.0]hexane[5]
1-Biphenyl-4-yl-3-aza-bicyclo[3.1.0]hexane[5]
1-Methyl-2- (4-phenylsulfanyl-phenyl)-ethylamine[7]
1-Methyl-4-p-tolyl-piperidine-4-carbonitrile[8]
1-benzylpiperidine hydrochloride[9]
1-fluoro-5-phenyl-3-aza-bicyclo[3.1.0]hexane[5]
1-phenyl-3-aza-bicyclo[3.1.0]hexane[5]
10R-hydroxylobel-7-ene[10]
10R-hydroxylobelane[10]
10S-hydroxylobel-7-ene[10]
10S-hydroxylobelane[10]
1S,2R-milnacipran[11]
2- (3-Methyl-piperazin-1-yl)-6-nitro-quinoline[12]
2-Amino-1- (4-ethylthiophenyl)butane[7]
2-Amino-1- (4-ethylthiophenyl)propane[7]
2-Amino-1- (4-methylthiophenyl)butane[7]
2-Amino-1- (4-methylthiophenyl)propane[7]
2-N,N-Dimethylamino-1- (4-methylthiophenyl)propane[7]
2-N- (Isopropyl)amino-1-[7]
2-N- (n-Propyl)amino-1-[7]
2-N-Allylamino-1- (4-methylthiophenyl)propan[7]
2-N-Cyclopropylamino-1- (4-methylthiophenyl)butane[7]
2-N-Ethylamino-1- (4-ethylthiophenyl)butane[7]
2-N-Ethylamino-1- (4-ethylthiophenyl)propane[7]
2-N-Ethylamino-1- (4-methylthiophenyl)butane[7]
2-N-Ethylamino-1- (4-methylthiophenyl)propane[7]
2-N-Hydroxyamino-1- (4-ethylthiophenyl)butane[7]
2-N-Hydroxyamino-1- (4-ethylthiophenyl)propane[7]
2-N-Hydroxyamino-1- (4-methylthiophenyl)butane[7]
2-N-Hydroxyamino-1- (4-methylthiophenyl)propane[7]
2-N-Methoxyamino-1- (4-methylthiophenyl)propane[7]
2-N-Methylamino-1- (4-ethylthiophenyl)propane[7]
2-N-Methylamino-1- (4-methylthiophenyl)butane[7]
2-N-Methylamino-1- (4-methylthiophenyl)propane[7]
2-N-Propargylamino-1- (4-methylthiophenyl)butane[7]
2-N-Propargylamino-1- (4-methylthiophenyl)propane[7]
2-Naphthalen-2-ylmethyl-4,5-dihydro-1H-imidazole[13]
2-[1,4]Diazepan-1-yl-6-nitro-quinoline[12]
3- (3,4-dichlorophenyl)-2-nortropene[14]
3- (4-Chlorophenyl)-2-nortropene[14]
3- (4-Fluorophenyl)-2-nortropene[14]
3- (4-Trifluoromethylphenyl)-2-nortropene[14]
3-Bromo-6-nitro-2-piperazin-1-yl-quinoline[12]
3-Phenyl-2-nortropene[14]
3-alpha-Phenylmethoxy-3-beta-phenyl-nortropane[14]
3-p-Tolyl-8-aza-bicyclo[3.2.1]octane[15]
3alpha- (bis-chloro-phenylmethoxy)tropane[16]
4-Allyl-6-nitro-2-piperazin-1-yl-quinoline[17]
4-Benzyl-6-nitro-2-piperazin-1-yl-quinoline[17]
4-Bromo-6-nitro-2-piperazin-1-yl-quinoline[17]
4-Chloro-6-nitro-2-piperazin-1-yl-quinoline[17]
4-Furan-2-yl-6-nitro-2-piperazin-1-yl-quinoline[17]
4-Iodo-6-nitro-2-piperazin-1-yl-quinoline[17]
6,6-dimethyl-1-phenyl-3-aza-bicyclo[3.1.0]hexane[5]
6,8-Dinitro-2-piperazin-1-yl-quinoline[12]
6- (3-aza-bicyclo[3.1.0]hexan-1-yl)quinoline[5]
6-Bromo-2-piperazin-1-yl-quinoline[12]
6-Chloro-2-piperazin-1-yl-quinoline[12]
6-Iodo-2-piperazin-1-yl-quinoline[12]
6-Nitro-2-piperazin-1-yl-4-vinyl-quinoline[17]
6-Nitro-4-phenyl-2-piperazin-1-yl-quinoline[17]
6-nitroquipazine[18]
8-Methyl-3-p-tolyl-8-aza-bicyclo[3.2.1]octane[15]
8R-hydroxylobel-9-ene[19]
8R-hydroxylobelane[10]
8S-hydroxylobel-9-ene[10]
8S-hydroxylobelane[10]
A-80426[13]
COCAINE.HCL[9]
Cyclohexyl- (3,4-dichloro-phenyl)-acetonitrile[20]
Cyclopentyl- (3,4-dichloro-phenyl)-acetonitrile[20]
D-166A[21]
D-211A[21]
D-211B[21]
D-254C[21]
D-257A[21]
D-257C[21]
DIFLUOROBENZTROPINE[16]
FLUOXETINE HYDROCHLORIDE[22]
GBR-12909[23]
Irindalone[24]
METHYLENEDIOXYAMPHETAMINE[7]
METHYLENEDIOXYMETHAMPHETAMINE[7]
N*1*- (6-Nitro-quinolin-2-yl)-ethane-1,2-diamine[12]
NISOXETINE[4]
QUIPAZINE[12]
TEFLUDAZINE[25]
WIN-35065[26]
WIN-35065-2[27]
WIN_35428[27]
ZIMELIDINE[28]
[3- (3,4-Dichloro-phenyl)-indan-1-yl]-methyl-amine[6]
erythro-3,4-dichloromethylphenidate hydrochloride[9]
para-Methoxyamphetamine[7]
para-chloroamphetamine[7]
threo-1-aza-5-phenyl[4.4.0]decane hydrochloride[9]
threo-3,4-dichlororitalinol hydrochloride[9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Evaluation of antidepressant-related behavioral responses in mice lacking the serotonin transporter. Neuropsychopharmacology. 2002 Dec;27(6):914-23. To Reference
Ref 2Bioorg Med Chem Lett. 2008 Sep 15;18(18):4940-3. Epub 2008 Aug 19.New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter. To Reference
Ref 3Bioorg 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. To Reference
Ref 4Bioorg 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. To Reference
Ref 5Bioorg 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. To Reference
Ref 6J 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. To Reference
Ref 7Eur 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. To Reference
Ref 8Bioorg Med Chem Lett. 1999 Dec 6;9(23):3273-6.Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine. To Reference
Ref 9J 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. To Reference
Ref 10Bioorg 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. To Reference
Ref 11J 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. To Reference
Ref 12Bioorg Med Chem Lett. 2000 Jul 17;10(14):1559-62.Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1. To Reference
Ref 13J 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 inhibiting and alpha2-antagonistic activities. To Reference
Ref 14Bioorg Med Chem Lett. 2009 Dec 15;19(24):6865-8. Epub 2009 Oct 23.Synthesis and monoamine transporter affinity of 3alpha-arylmethoxy-3beta-arylnortropanes. To Reference
Ref 15Bioorg 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. To Reference
Ref 16J 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. To Reference
Ref 17Bioorg 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. To Reference
Ref 18Bioorg 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. To Reference
Ref 19Bioorg 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. To Reference
Ref 20J 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. To Reference
Ref 21Bioorg 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. To Reference
Ref 22Bioorg Med Chem. 2010 Dec 1;18(23):8356-64. Epub 2010 Sep 29.Synthesis and structure-activity studies of benzyl ester meperidine and normeperidine derivatives as selective serotonin transporter ligands. To Reference
Ref 23Bioorg Med Chem Lett. 2008 Oct 1;18(19):5238-41. Epub 2008 Aug 22.Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol. To Reference
Ref 24J Med Chem. 1988 Dec;31(12):2247-56.Antihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity. To Reference
Ref 25J Med Chem. 1983 Jul;26(7):935-47.Neuroleptic activity and dopamine-uptake inhibition in 1-piperazino-3-phenylindans. To Reference
Ref 26J 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]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes. To Reference
Ref 27J 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. To Reference
Ref 28J Med Chem. 1984 Nov;27(11):1508-15.Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins. To Reference



 

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