Proteins > Sodium-dependent dopamine transporter
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Sodium-dependent dopamine transporter
A sodium-dependent dopamine transporter that is encoded in the genome of rat. [OMA:P23977, PRO:DNx]
Synonyms
DA transporter;
DAT;
Solute carrier family 6 member 3
Research
Bioassay Publications (136)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 4 (2.94) | 18.7374 |
| 1990's | 48 (35.29) | 18.2507 |
| 2000's | 65 (47.79) | 29.6817 |
| 2010's | 17 (12.50) | 24.3611 |
| 2020's | 2 (1.47) | 2.80 |
Compounds (134)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bupropion | Rattus norvegicus (Norway rat) | Ki | 0.3715 | 1 | 1 |
| 7-hydroxy-2-n,n-dipropylaminotetralin | Rattus norvegicus (Norway rat) | Ki | 0.0029 | 1 | 1 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 3 |
| 8-hydroxy-2-(di-n-propylamino)tetralin | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 1 | 1 |
| 1-(1-naphthyl)piperazine | Rattus norvegicus (Norway rat) | Ki | 0.0400 | 1 | 1 |
| 3-[(4-chlorophenyl)-phenylmethoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Rattus norvegicus (Norway rat) | Ki | 0.2360 | 3 | 4 |
| methylbufotenin | Rattus norvegicus (Norway rat) | Ki | 0.0160 | 1 | 1 |
| tacrine | Rattus norvegicus (Norway rat) | IC50 | 22.0000 | 1 | 1 |
| carbetapentane | Rattus norvegicus (Norway rat) | Ki | 3.0903 | 1 | 1 |
| chlorpromazine | Rattus norvegicus (Norway rat) | IC50 | 1.4791 | 1 | 2 |
| chlorpromazine | Rattus norvegicus (Norway rat) | Ki | 0.0040 | 1 | 1 |
| cisapride | Rattus norvegicus (Norway rat) | IC50 | 0.0065 | 1 | 2 |
| citalopram | Rattus norvegicus (Norway rat) | IC50 | 41.0000 | 1 | 1 |
| desipramine | Rattus norvegicus (Norway rat) | IC50 | 7.8000 | 1 | 1 |
| desipramine | Rattus norvegicus (Norway rat) | Ki | 7.0000 | 2 | 2 |
| amphetamine | Rattus norvegicus (Norway rat) | IC50 | 0.9600 | 1 | 1 |
| fluoxetine | Rattus norvegicus (Norway rat) | IC50 | 6.0000 | 1 | 1 |
| fluoxetine | Rattus norvegicus (Norway rat) | Ki | 1.0920 | 1 | 1 |
| vanoxerine | Rattus norvegicus (Norway rat) | IC50 | 0.0103 | 19 | 20 |
| vanoxerine | Rattus norvegicus (Norway rat) | Ki | 0.0129 | 14 | 19 |
| gbr 12935 | Rattus norvegicus (Norway rat) | IC50 | 0.0038 | 5 | 5 |
| gbr 12935 | Rattus norvegicus (Norway rat) | Ki | 0.0662 | 6 | 10 |
| granisetron | Rattus norvegicus (Norway rat) | IC50 | 3.8019 | 1 | 2 |
| haloperidol | Rattus norvegicus (Norway rat) | Ki | 3.0000 | 2 | 2 |
| velnacrine | Rattus norvegicus (Norway rat) | IC50 | 20.0000 | 1 | 1 |
| imipramine | Rattus norvegicus (Norway rat) | IC50 | 3.3884 | 1 | 2 |
| indomethacin | Rattus norvegicus (Norway rat) | IC50 | 14.0000 | 1 | 1 |
| loxapine | Rattus norvegicus (Norway rat) | Ki | 0.0150 | 1 | 1 |
| mazindol | Rattus norvegicus (Norway rat) | IC50 | 0.0454 | 9 | 12 |
| mazindol | Rattus norvegicus (Norway rat) | Ki | 0.0393 | 3 | 3 |
| meperidine | Rattus norvegicus (Norway rat) | Ki | 17.8000 | 1 | 1 |
| methiothepin | Rattus norvegicus (Norway rat) | Ki | 0.1000 | 1 | 1 |
| methylphenidate | Rattus norvegicus (Norway rat) | IC50 | 0.0830 | 1 | 1 |
| mirtazapine | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 3 |
| modafinil | Rattus norvegicus (Norway rat) | IC50 | 3.9167 | 6 | 6 |
| modafinil | Rattus norvegicus (Norway rat) | Ki | 5.9800 | 2 | 2 |
| nisoxetine | Rattus norvegicus (Norway rat) | IC50 | 0.3771 | 2 | 4 |
| nomifensine | Rattus norvegicus (Norway rat) | IC50 | 0.1642 | 6 | 6 |
| nomifensine | Rattus norvegicus (Norway rat) | Ki | 0.0343 | 2 | 2 |
| oxidopamine | Rattus norvegicus (Norway rat) | Ki | 0.0120 | 1 | 1 |
| perhexiline | Rattus norvegicus (Norway rat) | IC50 | 7.7625 | 1 | 2 |
| risperidone | Rattus norvegicus (Norway rat) | Ki | 0.0310 | 1 | 2 |
| spiperone | Rattus norvegicus (Norway rat) | Ki | 0.5329 | 2 | 3 |
| terfenadine | Rattus norvegicus (Norway rat) | IC50 | 0.1288 | 1 | 2 |
| thioridazine | Rattus norvegicus (Norway rat) | IC50 | 0.0355 | 1 | 2 |
| u 99194 | Rattus norvegicus (Norway rat) | Ki | 0.0310 | 1 | 1 |
| venlafaxine | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 3 |
| zonisamide | Rattus norvegicus (Norway rat) | Ki | 0.0352 | 1 | 1 |
| meperidine hydrochloride | Rattus norvegicus (Norway rat) | Ki | 17.8000 | 1 | 1 |
| lysergic acid diethylamide | Rattus norvegicus (Norway rat) | Ki | 0.0100 | 1 | 1 |
| caramiphen | Rattus norvegicus (Norway rat) | Ki | 5.2481 | 1 | 1 |
| taurocholic acid | Rattus norvegicus (Norway rat) | IC50 | 6.0000 | 1 | 1 |
| ergotamine | Rattus norvegicus (Norway rat) | Ki | 0.0400 | 1 | 1 |
| benzoin | Rattus norvegicus (Norway rat) | Ki | 7.2100 | 1 | 1 |
| benzil | Rattus norvegicus (Norway rat) | Ki | 0.0451 | 1 | 1 |
| liriodenine | Rattus norvegicus (Norway rat) | IC50 | 31.0000 | 1 | 1 |
| 2-bromolysergic acid diethylamide | Rattus norvegicus (Norway rat) | Ki | 0.0100 | 1 | 1 |
| alpha-naphthoflavone | Rattus norvegicus (Norway rat) | IC50 | 0.0100 | 1 | 1 |
| pimozide | Rattus norvegicus (Norway rat) | Ki | 0.0710 | 1 | 1 |
| laurolitsine | Rattus norvegicus (Norway rat) | IC50 | 16.5000 | 1 | 1 |
| talopram | Rattus norvegicus (Norway rat) | IC50 | 44.0000 | 1 | 1 |
| talopram | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| exp561 | Rattus norvegicus (Norway rat) | Ki | 0.0832 | 1 | 1 |
| talsupram | Rattus norvegicus (Norway rat) | IC50 | 9.3000 | 1 | 1 |
| 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 1 |
| paroxetine | Rattus norvegicus (Norway rat) | IC50 | 0.8492 | 2 | 5 |
| paroxetine | Rattus norvegicus (Norway rat) | Ki | 0.4000 | 1 | 1 |
| staurosporine | Rattus norvegicus (Norway rat) | IC50 | 0.0280 | 1 | 1 |
| rimcazole | Rattus norvegicus (Norway rat) | IC50 | 0.1400 | 1 | 1 |
| rimcazole | Rattus norvegicus (Norway rat) | Ki | 0.1644 | 2 | 2 |
| quinpirole | Rattus norvegicus (Norway rat) | Ki | 0.0240 | 1 | 2 |
| atomoxetine | Rattus norvegicus (Norway rat) | IC50 | 2.0000 | 1 | 1 |
| atomoxetine | Rattus norvegicus (Norway rat) | Ki | 0.7080 | 1 | 1 |
| (S)-nomifensine | Rattus norvegicus (Norway rat) | IC50 | 0.0480 | 1 | 1 |
| duloxetine | Rattus norvegicus (Norway rat) | IC50 | 0.3700 | 1 | 1 |
| ziprasidone | Rattus norvegicus (Norway rat) | IC50 | 0.1514 | 1 | 2 |
| mizolastine | Rattus norvegicus (Norway rat) | IC50 | 0.3548 | 1 | 2 |
| sertraline | Rattus norvegicus (Norway rat) | IC50 | 0.8250 | 1 | 1 |
| diclofensine | Rattus norvegicus (Norway rat) | Ki | 0.0071 | 1 | 1 |
| fluoren-9-ol | Rattus norvegicus (Norway rat) | IC50 | 9.0000 | 1 | 1 |
| tryptoline | Rattus norvegicus (Norway rat) | Ki | 5.0000 | 1 | 1 |
| gr 113808 | Rattus norvegicus (Norway rat) | Ki | 0.0004 | 3 | 5 |
| gefitinib | Rattus norvegicus (Norway rat) | IC50 | 0.2810 | 1 | 1 |
| 1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine | Rattus norvegicus (Norway rat) | IC50 | 0.0164 | 9 | 10 |
| 1-(1-(2-benzo(b)thienyl)cyclohexyl)piperidine | Rattus norvegicus (Norway rat) | Ki | 0.0100 | 1 | 1 |
| 2,4,5-trihydroxyamphetamine | Rattus norvegicus (Norway rat) | Ki | 0.0160 | 1 | 1 |
| indatraline | Rattus norvegicus (Norway rat) | Ki | 0.0230 | 1 | 1 |
| pre 084 | Rattus norvegicus (Norway rat) | Ki | 5.3703 | 1 | 1 |
| tamsulosin | Rattus norvegicus (Norway rat) | Ki | 0.0780 | 1 | 1 |
| 5-amino-2,4-dihydroxy-alpha-methylphenylethylamine | Rattus norvegicus (Norway rat) | Ki | 0.1120 | 1 | 1 |
| 4-hydroxy-2-(di-n-propylamino)indan | Rattus norvegicus (Norway rat) | Ki | 0.0420 | 1 | 1 |
| 2-iodolysergic acid diethylamide | Rattus norvegicus (Norway rat) | Ki | 0.0100 | 1 | 1 |
| dexmethylphenidate hydrochloride | Rattus norvegicus (Norway rat) | Ki | 0.0746 | 1 | 1 |
| dexmethylphenidate | Rattus norvegicus (Norway rat) | IC50 | 0.0358 | 2 | 5 |
| anonaine | Rattus norvegicus (Norway rat) | IC50 | 0.8000 | 1 | 1 |
| 6-aminodopamine | Rattus norvegicus (Norway rat) | Ki | 0.0170 | 1 | 1 |
| 5-hydroxy-2-n,n-dipropylaminotetralin | Rattus norvegicus (Norway rat) | Ki | 0.0007 | 1 | 3 |
| erlotinib | Rattus norvegicus (Norway rat) | IC50 | 0.3690 | 1 | 1 |
| cocaine | Rattus norvegicus (Norway rat) | IC50 | 1.3496 | 47 | 67 |
| cocaine | Rattus norvegicus (Norway rat) | Ki | 25.8768 | 25 | 40 |
| jp-1302 | Rattus norvegicus (Norway rat) | Ki | 3.2000 | 1 | 1 |
| tropacocaine | Rattus norvegicus (Norway rat) | IC50 | 31.5985 | 10 | 13 |
| cocaine hydrochloride | Rattus norvegicus (Norway rat) | Ki | 0.1560 | 1 | 1 |
| chlorprothixene | Rattus norvegicus (Norway rat) | Ki | 0.0030 | 1 | 1 |
| levosulpiride | Rattus norvegicus (Norway rat) | Ki | 0.0510 | 1 | 1 |
| benztropine | Rattus norvegicus (Norway rat) | Ki | 0.1202 | 4 | 4 |
| (R)-fluoxetine | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 3 |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Rattus norvegicus (Norway rat) | IC50 | 1.0000 | 1 | 3 |
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 1 | 1 |
| amiflamine | Rattus norvegicus (Norway rat) | IC50 | 10.0000 | 1 | 1 |
| n,n-dimethylepinephrine | Rattus norvegicus (Norway rat) | IC50 | 949.0000 | 1 | 1 |
| n,n-dimethylepinephrine | Rattus norvegicus (Norway rat) | Ki | 530.0000 | 1 | 1 |
| sb 258585 | Rattus norvegicus (Norway rat) | Ki | 0.0025 | 1 | 1 |
| rs-130830 | Rattus norvegicus (Norway rat) | IC50 | 0.0140 | 1 | 1 |
| 3-[bis(4-fluorophenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Rattus norvegicus (Norway rat) | IC50 | 0.0138 | 1 | 1 |
| 3-[bis(4-fluorophenyl)methoxy]-8-methyl-8-azabicyclo[3.2.1]octane | Rattus norvegicus (Norway rat) | Ki | 0.0236 | 4 | 5 |
| quercetin | Rattus norvegicus (Norway rat) | IC50 | 20.0000 | 1 | 1 |
| l 745870 | Rattus norvegicus (Norway rat) | Ki | 10.0000 | 2 | 3 |
| ml 10302 | Rattus norvegicus (Norway rat) | Ki | 0.0092 | 3 | 5 |
| ro 63-0563 | Rattus norvegicus (Norway rat) | Ki | 0.0126 | 1 | 1 |
| ro 4-6790 | Rattus norvegicus (Norway rat) | Ki | 0.0501 | 1 | 1 |
| sb 271046 | Rattus norvegicus (Norway rat) | Ki | 0.0012 | 2 | 4 |
| bisdemethoxycurcumin | Rattus norvegicus (Norway rat) | IC50 | 36.3700 | 1 | 1 |
| 7-hydroxy-2-(n-n-propyl-n-(3-iodo-2'-propenyl)-amino)tetralin | Rattus norvegicus (Norway rat) | Ki | 0.0018 | 1 | 1 |
| 2-ethyl-5-methoxy-n,n-dimethyltryptamine | Rattus norvegicus (Norway rat) | Ki | 0.0160 | 1 | 1 |
| 5-methoxy-2-phenyl-n,n-dimethyltryptamine | Rattus norvegicus (Norway rat) | Ki | 0.0200 | 1 | 1 |
| ms-245 | Rattus norvegicus (Norway rat) | Ki | 0.0022 | 1 | 2 |
| n-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | Rattus norvegicus (Norway rat) | Ki | 0.0030 | 1 | 1 |
| dov 216303 | Rattus norvegicus (Norway rat) | IC50 | 0.0215 | 1 | 2 |
| sr 147778 | Rattus norvegicus (Norway rat) | Ki | 0.4420 | 1 | 1 |
| methyl 4-(4-chlorophenyl)-1-methylpiperidine-3-carboxylate | Rattus norvegicus (Norway rat) | Ki | 0.2442 | 2 | 4 |
| n,n-dimethyl-2-(2-amino-4-methylphenylthio)benzylamine | Rattus norvegicus (Norway rat) | Ki | 1.0000 | 1 | 2 |
| 77-lh-28-1 | Rattus norvegicus (Norway rat) | Ki | 3.3884 | 1 | 1 |
| methyl 4-(4-chlorophenyl)-1-methylpiperidine-3-carboxylate | Rattus norvegicus (Norway rat) | IC50 | 0.1624 | 2 | 3 |
| methyl 4-(4-chlorophenyl)-1-methylpiperidine-3-carboxylate | Rattus norvegicus (Norway rat) | Ki | 0.2605 | 3 | 3 |
| milnacipran | Rattus norvegicus (Norway rat) | IC50 | 37.0000 | 1 | 1 |
| 2-((2-((dimethylamino)methyl)phenyl)thio)-5-iodophenylamine | Rattus norvegicus (Norway rat) | Ki | 0.8997 | 2 | 3 |
| gdc 0449 | Rattus norvegicus (Norway rat) | IC50 | 0.0200 | 1 | 1 |
| niraparib | Rattus norvegicus (Norway rat) | IC50 | 0.0021 | 1 | 1 |
| niraparib | Rattus norvegicus (Norway rat) | Ki | 0.0040 | 1 | 1 |
| (1R,3S)-3-(4-iodophenyl)-8-methyl-8-azabicyclo[3.2.1]octane-4-carboxylic acid methyl ester | Rattus norvegicus (Norway rat) | IC50 | 0.0012 | 4 | 4 |
| win 35,065-2 | Rattus norvegicus (Norway rat) | IC50 | 0.0230 | 1 | 2 |
| win 35,065-2 | Rattus norvegicus (Norway rat) | Ki | 0.0871 | 1 | 1 |
| anagliptin | Rattus norvegicus (Norway rat) | IC50 | 72.7000 | 1 | 1 |
| clozapine | Rattus norvegicus (Norway rat) | IC50 | 5.7544 | 1 | 2 |
| clozapine | Rattus norvegicus (Norway rat) | Ki | 0.2392 | 4 | 5 |
| hydrazinocurcumin | Rattus norvegicus (Norway rat) | IC50 | 9.7000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| n,n-dimethylepinephrine | Rattus norvegicus (Norway rat) | Km | 1,400.0000 | 1 | 1 |
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
A two-state homology model of the hERG K+ channel: application to ligand binding.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.Bioorganic & medicinal chemistry letters, , May-16, Volume: 15, Issue:10, 2005
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
9-Amino-1,2,3,4-tetrahydroacridin-1-ols: synthesis and evaluation as potential Alzheimer's disease therapeutics.Journal of medicinal chemistry, , Volume: 32, Issue:8, 1989
Flexible and biomimetic analogs of triple uptake inhibitor 4-((((3S,6S)-6-benzhydryltetrahydro-2H-pyran-3-yl)amino)methyl)phenol: Synthesis, biological characterization, and development of a pharmacophore model.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, mJournal of medicinal chemistry, , May-08, Volume: 51, Issue:9, 2008
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.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Discovery of novel trisubstituted asymmetric derivatives of (2S,4R,5R)-2-benzhydryl-5-benzylaminotetrahydropyran-4-ol, exhibiting high affinity for serotonin and norepinephrine transporters in a stereospecific manner.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.Journal of medicinal chemistry, , Dec-02, Volume: 47, Issue:25, 2004
Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Structure-activity relationship studies of highly selective inhibitors of the dopamine transporter: N-benzylpiperidine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Development of long-acting dopamine transporter ligands as potential cocaine-abuse therapeutic agents: chiral hydroxyl-containing derivatives of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-pheJournal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Synthesis and transporter binding properties of bridged piperazine analogues of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909).Journal of medicinal chemistry, , Dec-14, Volume: 43, Issue:25, 2000
Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.Journal of medicinal chemistry, , Dec-02, Volume: 42, Issue:24, 1999
Design and synthesis of a biotinylated dopamine transporter ligand for the purification and labeling of dopaminergic neurons.Bioorganic & medicinal chemistry letters, , Feb-03, Volume: 8, Issue:3, 1998
Highly selective, novel analogs of 4-[2-(diphenylmethoxy)ethyl]- 1-benzylpiperidine for the dopamine transporter: effect of different aromatic substitutions on their affinity and selectivity.Journal of medicinal chemistry, , Jan-03, Volume: 40, Issue:1, 1997
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).Journal of medicinal chemistry, , Nov-22, Volume: 39, Issue:24, 1996
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Design and synthesis of 2- and 3-substituted-3-phenylpropyl analogs of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine: role of amino, fluoro, hydroxyl, methoxyl, methyl, mJournal of medicinal chemistry, , May-08, Volume: 51, Issue:9, 2008
Further exploration of 1-[2-[Bis-(4-fluorophenyl)methoxy]ethyl]piperazine (GBR 12909): role of N-aromatic, N-heteroaromatic, and 3-oxygenated N-phenylpropyl substituents on affinity for the dopamine and serotonin transporter.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 13, Issue:7, 2003
Development of long-acting dopamine transporter ligands as potential cocaine-abuse therapeutic agents: chiral hydroxyl-containing derivatives of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine and 1-[2-(diphenylmethoxy)ethyl]-4-(3-pheJournal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Oxygenated analogues of 1-[2-(Diphenylmethoxy)ethyl]- and 1-[2-[Bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as potential extended-action cocaine-abuse therapeutic agents.Journal of medicinal chemistry, , Dec-02, Volume: 42, Issue:24, 1999
Design and synthesis of a biotinylated dopamine transporter ligand for the purification and labeling of dopaminergic neurons.Bioorganic & medicinal chemistry letters, , Feb-03, Volume: 8, Issue:3, 1998
Heteroaromatic analogs of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909) as high-affinity dopamine reuptake inhibitors.Journal of medicinal chemistry, , Feb-28, Volume: 40, Issue:5, 1997
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).Journal of medicinal chemistry, , Nov-22, Volume: 39, Issue:24, 1996
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Benzo- and cyclohexanomazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
Wake-promoting agents: search for next generation modafinil: part I.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 22, Issue:6, 2012
Wake promoting agents: search for next generation modafinil, lessons learned: part III.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 22, Issue:11, 2012
Wake-promoting agents: search for next generation modafinil: part IV.European journal of medicinal chemistry, , Volume: 54, 2012
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.Bioorganic & medicinal chemistry, , Jan-01, Volume: 19, Issue:1, 2011
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Spiperone: influence of spiro ring substituents on 5-HT2A serotonin receptor binding.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Illuminating the norepinephrine transporter: fluorescent probes based on nisoxetine and talopram.RSC medicinal chemistry, , Jul-21, Volume: 12, Issue:7, 2021
3-Phenyl-1-indanamines. Potential antidepressant activity and potent inhibition of dopamine, norepinephrine, and serotonin uptake.Journal of medicinal chemistry, , Volume: 28, Issue:12, 1985
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Synthesis and ligand binding of tropane ring analogues of paroxetine.Journal of medicinal chemistry, , Jan-15, Volume: 41, Issue:2, 1998
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Cyclic amidines as benzamide bioisosteres: EPC synthesis and SAR studies leading to the selective dopamine D4 receptor agonist FAUC 312.Bioorganic & medicinal chemistry letters, , Mar-10, Volume: 13, Issue:5, 2003
Synthesis and pharmacological evaluation of thiopyran analogues of the dopamine D3 receptor-selective agonist (4aR,10bR)-(+)-trans-3,4,4a,10b-tetrahydro-4-n-propyl-2H,5H [1]b enzopyrano[4,3-b]-1,4-oxazin-9-ol (PD 128907).Journal of medicinal chemistry, , Jul-27, Volume: 43, Issue:15, 2000
1-Naphthyl and 4-indolyl arylalkylamines as selective monoamine reuptake inhibitors.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
1-[1-2-Benzo[b]thiopheneyl)cyclohexyl]piperidine hydrochloride (BTCP) yields two active primary metabolites in vitro: synthesis, identification from rat liver microsome extracts, and affinity for the neuronal dopamine transporter.Journal of medicinal chemistry, , Dec-05, Volume: 40, Issue:25, 1997
Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites.Journal of medicinal chemistry, , Dec-10, Volume: 36, Issue:25, 1993
Synthesis and biological evaluation of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine homologues at dopamine-uptake and phencyclidine- and sigma-binding sites.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Localization of cocaine analog [125I]RTI 82 irreversible binding to transmembrane domain 6 of the dopamine transporter.The Journal of biological chemistry, , Mar-23, Volume: 282, Issue:12, 2007
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.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
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.Journal of medicinal chemistry, , Oct-19, Volume: 49, Issue:21, 2006
Development of peptidic dopamine transporter inhibitors via aromatic modification-mediated conformational restriction.Journal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
A two-state homology model of the hERG K+ channel: application to ligand binding.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds.Journal of medicinal chemistry, , Jun-02, Volume: 48, Issue:11, 2005
Synthesis and biological evaluation of meperidine analogues at monoamine transporters.Journal of medicinal chemistry, , Mar-10, Volume: 48, Issue:5, 2005
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.Journal of medicinal chemistry, , Sep-12, Volume: 45, Issue:19, 2002
Identification of a novel partial inhibitor of dopamine transporter among 4-substituted 2-phenylquinazolines.Bioorganic & medicinal chemistry letters, , Aug-19, Volume: 12, Issue:16, 2002
SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Synthesis and binding affinities of 2 beta-(3-iodoallyloxycarbonyl)-3 beta-(4-substituted-aryl)tropane analogues as ligands for the dopamine transporter studies.Bioorganic & medicinal chemistry letters, , Dec-03, Volume: 11, Issue:23, 2001
Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles.Bioorganic & medicinal chemistry letters, , Aug-20, Volume: 11, Issue:16, 2001
Pharmacophore-based discovery of 3,4-disubstituted pyrrolidines as a novel class of monoamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter.Journal of medicinal chemistry, , May-18, Volume: 43, Issue:10, 2000
3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter.Bioorganic & medicinal chemistry letters, , Nov-06, Volume: 10, Issue:21, 2000
Chemical synthesis and pharmacology of 6- and 7-hydroxylated 2-carbomethoxy-3-(p-tolyl)tropanes: antagonism of cocaine's locomotor stimulant effects.Journal of medicinal chemistry, , Aug-24, Volume: 43, Issue:17, 2000
Slow-onset, long-duration 3-(3',4'-dichlorophenyl)-1-indanamine monoamine reuptake blockers as potential medications to treat cocaine abuse.Journal of medicinal chemistry, , Dec-28, Volume: 43, Issue:26, 2000
Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Aug-07, Volume: 10, Issue:15, 2000
Discovery of a novel dopamine transporter inhibitor, 4-hydroxy-1-methyl-4-(4-methylphenyl)-3-piperidyl 4-methylphenyl ketone, as a potential cocaine antagonist through 3D-database pharmacophore searching. Molecular modeling, structure-activity relationshiJournal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Structure-activity relationships at the monoamine transporters and sigma receptors for a novel series of 9-[3-(cis-3, 5-dimethyl-1-piperazinyl)propyl]carbazole (rimcazole) analogues.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
N-phenylalkyl-substituted tropane analogs of boat conformation with high selectivity for the dopamine versus serotonin transporter.Bioorganic & medicinal chemistry letters, , Dec-06, Volume: 9, Issue:23, 1999
Synthesis and pharmacology of site-specific cocaine abuse treatment agents: 2-substituted-6-amino-5-phenylbicyclo[2.2.2]octanes.Journal of medicinal chemistry, , Nov-18, Volume: 42, Issue:23, 1999
(-)-3 beta-Substituted ecgonine methyl esters as inhibitors for cocaine binding and dopamine uptake.Journal of medicinal chemistry, , Mar-12, Volume: 41, Issue:6, 1998
Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
Synthesis and biological properties of new 2beta-alkyl- and 2beta-aryl-3-(substituted phenyl)tropane derivatives: stereochemical effect of C-3 on affinity and selectivity for neuronal dopamine and serotonin transporters.Journal of medicinal chemistry, , Dec-03, Volume: 41, Issue:25, 1998
Synthesis and transporter binding properties of (R)-2 beta, 3 beta- and (R)-2 alpha, 3 alpha-diaryltropanes.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 8, Issue:24, 1998
Synthesis and ligand binding studies of 4'-iodobenzoyl esters of tropanes and piperidines at the dopamine transporter.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
Synthesis and transporter binding properties of 2,3-diphenyltropane stereoisomers. Comparison to 3beta-phenyltropane-2beta-carboxylic acid esters.Journal of medicinal chemistry, , Apr-11, Volume: 40, Issue:8, 1997
Synthesis and transporter binding properties of 3 beta-(4'-alkyl-, 4'-alkenyl-, and 4'-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]-and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909).Journal of medicinal chemistry, , Nov-22, Volume: 39, Issue:24, 1996
3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter.Journal of medicinal chemistry, , Oct-11, Volume: 39, Issue:21, 1996
Synthesis and ligand binding study of 3 beta-(4'-substituted phenyl)-2 beta-(heterocyclic)tropanes.Journal of medicinal chemistry, , Sep-01, Volume: 38, Issue:18, 1995
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Cocaine and 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid ester and amide analogues. New high-affinity and selective compounds for the dopamine transporter.Journal of medicinal chemistry, , Jan-20, Volume: 38, Issue:2, 1995
Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters.Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Synthesis of substituted 3-carbamoylecgonine methyl ester analogues: irreversible and photoaffinity ligands for the cocaine receptor/dopamine transporter.Journal of medicinal chemistry, , Jul-08, Volume: 37, Issue:14, 1994
Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding.Journal of medicinal chemistry, , Sep-30, Volume: 37, Issue:20, 1994
Synthesis and characterization of radioiodinated N-(3-iodopropen-1-yl)-2 beta-carbomethoxy-3 beta-(4-chlorophenyl)tropanes: potential dopamine reuptake site imaging agents.Journal of medicinal chemistry, , May-13, Volume: 37, Issue:10, 1994
Analysis of cocaine receptor site ligand binding by three-dimensional Voronoi site modeling approach.Journal of medicinal chemistry, , Nov-12, Volume: 36, Issue:23, 1993
Further studies of the structure-activity relationships of 1-[1-(2-benzo[b]thienyl)cyclohexyl]piperidine. Synthesis and evaluation of 1-(2-benzo[b]thienyl)-N,N-dialkylcyclohexylamines at dopamine uptake and phencyclidine binding sites.Journal of medicinal chemistry, , Dec-10, Volume: 36, Issue:25, 1993
Probes for the cocaine receptor. Potentially irreversible ligands for the dopamine transporter.Journal of medicinal chemistry, , May-15, Volume: 35, Issue:10, 1992
Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter.Journal of medicinal chemistry, , Jun-26, Volume: 35, Issue:13, 1992
2 beta-substituted analogues of cocaine. Synthesis and inhibition of binding to the cocaine receptor.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
N-modified analogues of cocaine: synthesis and inhibition of binding to the cocaine receptor.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue.Journal of medicinal chemistry, , Dec-11, Volume: 35, Issue:25, 1992
Synthesis and receptor binding of N-substituted tropane derivatives. High-affinity ligands for the cocaine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:5, 1991
Synthesis and ligand binding of cocaine isomers at the cocaine receptor.Journal of medicinal chemistry, , Volume: 34, Issue:3, 1991
Analysis of cocaine receptor site ligand binding by three-dimensional Voronoi site modeling approach.Journal of medicinal chemistry, , Nov-12, Volume: 36, Issue:23, 1993
2 beta-substituted analogues of cocaine. Synthesis and inhibition of binding to the cocaine receptor.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
N-modified analogues of cocaine: synthesis and inhibition of binding to the cocaine receptor.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
3'-Chloro-3 alpha-(diphenylmethoxy)tropane but not 4'-chloro-3 alpha-(diphenylmethoxy)tropane produces a cocaine-like behavioral profile.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Flexible and biomimetic analogs of triple uptake inhibitor 4-((((3S,6S)-6-benzhydryltetrahydro-2H-pyran-3-yl)amino)methyl)phenol: Synthesis, biological characterization, and development of a pharmacophore model.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.Journal of medicinal chemistry, , Dec-04, Volume: 46, Issue:25, 2003
Structure-activity relationship comparison of (S)-2beta-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes and (R)-2beta-substituted 3beta-(3,4-dichlorophenyl)tropanes at the dopamine transporter.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Novel N-substituted 3 alpha-[bis(4'-fluorophenyl)methoxy]tropane analogues: selective ligands for the dopamine transporter.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Novel 4'-substituted and 4',4"-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.Journal of medicinal chemistry, , Sep-29, Volume: 38, Issue:20, 1995
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
Piperidine-based nocaine/modafinil hybrid ligands as highly potent monoamine transporter inhibitors: efficient drug discovery by rational lead hybridization.Journal of medicinal chemistry, , Nov-18, Volume: 47, Issue:24, 2004
Synthesis and biological evaluation of 1-azabicyclo-[3.2.1]octanes: new dopamine transporter inhibitors.Bioorganic & medicinal chemistry letters, , Aug-07, Volume: 10, Issue:15, 2000
Triple Reuptake Inhibitors as Potential Therapeutics for Depression and Other Disorders: Design Paradigm and Developmental Challenges.Journal of medicinal chemistry, , 03-22, Volume: 61, Issue:6, 2018
SAR studies of piperidine-based analogues of cocaine. 4. Effect of N-modification and ester replacement.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
Sar studies of piperidine-based analogues of cocaine. Part 3: oxadiazoles.Bioorganic & medicinal chemistry letters, , Aug-20, Volume: 11, Issue:16, 2001
Chemistry and pharmacology of the piperidine-based analogues of cocaine. Identification of potent DAT inhibitors lacking the tropane skeleton.Journal of medicinal chemistry, , May-21, Volume: 41, Issue:11, 1998
New PET imaging agent for the serotonin transporter: [(18)F]ACF (2-[(2-amino-4-chloro-5-fluorophenyl)thio]-N,N-dimethyl-benzenmethanamine).Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
Substituted diphenyl sulfides as selective serotonin transporter ligands: synthesis and in vitro evaluation.Journal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.Journal of medicinal chemistry, , May-08, Volume: 46, Issue:10, 2003
Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters.Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Synthesis, ligand binding, and QSAR (CoMFA and classical) study of 3 beta-(3'-substituted phenyl)-, 3 beta-(4'-substituted phenyl)-, and 3 beta-(3',4'-disubstituted phenyl)tropane-2 beta-carboxylic acid methyl esters.Journal of medicinal chemistry, , Sep-02, Volume: 37, Issue:18, 1994
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
2D QSAR modeling and preliminary database searching for dopamine transporter inhibitors using genetic algorithm variable selection of Molconn Z descriptors.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter.Journal of medicinal chemistry, , Jun-26, Volume: 35, Issue:13, 1992
A two-state homology model of the hERG K+ channel: application to ligand binding.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Part 1: identification and structure-activity relationships.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments.Journal of medicinal chemistry, , Nov-16, Volume: 43, Issue:23, 2000
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics. 2. Pharmacological profile of 7-[3-[4-(6-fluoro-1, 2-benzisoxazol-3-yl)-piperidin-1-yl]propoxy]-3-(hydroxymeth yl)chromen -4-one (abaperidone, FI-8602).Journal of medicinal chemistry, , Dec-31, Volume: 41, Issue:27, 1998