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1
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Structure of the human dopamine D3 receptor in complex with a D2/D3 selective antagonist.
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Science
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2010
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5.86
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2
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The binding sites for cocaine and dopamine in the dopamine transporter overlap.
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Nat Neurosci
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2008
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2.72
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3
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Relationship between conformational changes in the dopamine transporter and cocaine-like subjective effects of uptake inhibitors.
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Mol Pharmacol
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2007
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2.64
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4
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Yawning and hypothermia in rats: effects of dopamine D3 and D2 agonists and antagonists.
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Psychopharmacology (Berl)
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2007
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1.94
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5
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Novel heterocyclic trans olefin analogues of N-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl}arylcarboxamides as selective probes with high affinity for the dopamine D3 receptor.
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J Med Chem
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2005
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1.77
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6
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The novel dopamine D3 receptor antagonist NGB 2904 inhibits cocaine's rewarding effects and cocaine-induced reinstatement of drug-seeking behavior in rats.
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Neuropsychopharmacology
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2005
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1.69
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7
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Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists.
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Bioorg Med Chem Lett
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2007
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1.54
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8
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Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
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J Med Chem
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2007
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1.51
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9
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Identification of a dopamine transporter ligand that blocks the stimulant effects of cocaine.
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J Neurosci
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2005
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1.49
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10
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Effects of N-substituted analogs of benztropine: diminished cocaine-like effects in dopamine transporter ligands.
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J Pharmacol Exp Ther
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2004
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1.44
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11
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Acute administration of SB-277011A, NGB 2904, or BP 897 inhibits cocaine cue-induced reinstatement of drug-seeking behavior in rats: role of dopamine D3 receptors.
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Synapse
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2005
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1.43
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12
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Food restriction alters N'-propyl-4,5,6,7-tetrahydrobenzothiazole-2,6-diamine dihydrochloride (pramipexole)-induced yawning, hypothermia, and locomotor activity in rats: evidence for sensitization of dopamine D2 receptor-mediated effects.
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J Pharmacol Exp Ther
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2008
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1.31
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13
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Visualization of dopamine transporter trafficking in live neurons by use of fluorescent cocaine analogs.
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J Neurosci
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2009
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1.26
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14
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Effects of two novel D3-selective compounds, NGB 2904 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-9H-fluorene-2-carboxamide] and CJB 090 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridin-2-yl)benzamide], on the reinforcing and discriminative stimulus effects of cocaine in rhesus monkeys.
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J Pharmacol Exp Ther
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2007
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1.24
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15
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Dopamine transport inhibitors based on GBR12909 and benztropine as potential medications to treat cocaine addiction.
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Biochem Pharmacol
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2007
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1.20
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16
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N-(3-fluoro-4-(4-(2-methoxy or 2,3-dichlorophenyl)piperazine-1-yl)butyl)arylcarboxamides as selective dopamine D3 receptor ligands: critical role of the carboxamide linker for D3 receptor selectivity.
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J Med Chem
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2011
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1.20
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17
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Postendocytic sorting of constitutively internalized dopamine transporter in cell lines and dopaminergic neurons.
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J Biol Chem
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2010
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1.17
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18
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Recognition of benztropine by the dopamine transporter (DAT) differs from that of the classical dopamine uptake inhibitors cocaine, methylphenidate, and mazindol as a function of a DAT transmembrane 1 aspartic acid residue.
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J Pharmacol Exp Ther
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2005
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1.14
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19
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Combinations of cocaine with other dopamine uptake inhibitors: assessment of additivity.
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J Pharmacol Exp Ther
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2009
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1.13
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20
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PG01037, a novel dopamine D3 receptor antagonist, inhibits the effects of methamphetamine in rats.
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J Psychopharmacol
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2010
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1.13
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21
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R-modafinil (armodafinil): a unique dopamine uptake inhibitor and potential medication for psychostimulant abuse.
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Biol Psychiatry
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2012
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1.12
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22
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The binding sites for benztropines and dopamine in the dopamine transporter overlap.
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Neuropharmacology
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2010
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1.11
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23
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Dopamine D3 and D2 receptor mechanisms in the abuse-related behavioral effects of cocaine: studies with preferential antagonists in squirrel monkeys.
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J Pharmacol Exp Ther
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2010
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1.09
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24
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Steric hindrance mutagenesis in the conserved extracellular vestibule impedes allosteric binding of antidepressants to the serotonin transporter.
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J Biol Chem
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2012
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1.09
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25
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Rhodamine-labeled 2beta-carbomethoxy-3beta-(3,4-dichlorophenyl)tropane analogues as high-affinity fluorescent probes for the dopamine transporter.
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J Med Chem
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2005
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1.07
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26
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Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.
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Bioorg Med Chem Lett
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2006
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1.04
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27
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Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.
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Bioorg Med Chem Lett
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2007
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1.04
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28
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Labeling of dopamine transporter transmembrane domain 1 with the tropane ligand N-[4-(4-azido-3-[125I]iodophenyl)butyl]-2beta-carbomethoxy-3beta-(4-chlorophenyl)tropane implicates proximity of cocaine and substrate active sites.
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Mol Pharmacol
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2008
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1.03
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29
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Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.
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J Med Chem
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2009
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1.03
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30
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The neurobiology of modafinil as an enhancer of cognitive performance and a potential treatment for substance use disorders.
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Psychopharmacology (Berl)
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2013
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1.02
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31
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N-substituted benztropine analogs: selective dopamine transporter ligands with a fast onset of action and minimal cocaine-like behavioral effects.
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J Pharmacol Exp Ther
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2010
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1.01
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32
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Assessment of the influence of histaminergic actions on cocaine-like effects of 3alpha-diphenylmethoxytropane analogs.
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J Pharmacol Exp Ther
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2005
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1.00
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33
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Evaluation of the blood-brain barrier transport, population pharmacokinetics, and brain distribution of benztropine analogs and cocaine using in vitro and in vivo techniques.
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J Pharmacol Exp Ther
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2003
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1.00
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34
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Evaluation of the D3 dopamine receptor selective antagonist PG01037 on L-dopa-dependent abnormal involuntary movements in rats.
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Neuropharmacology
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2009
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0.98
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35
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Behavioral effects of rimcazole analogues alone and in combination with cocaine.
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Eur J Pharmacol
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2003
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0.97
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36
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Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists.
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Bioorg Med Chem Lett
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2006
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0.96
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37
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Proerectile effects of dopamine D2-like agonists are mediated by the D3 receptor in rats and mice.
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J Pharmacol Exp Ther
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2009
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0.96
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38
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Place conditioning and locomotor effects of N-substituted, 4',4''-difluorobenztropine analogs in rats.
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J Pharmacol Exp Ther
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2005
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0.94
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39
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Probing binding pocket of serotonin transporter by single molecular force spectroscopy on living cells.
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J Biol Chem
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2011
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0.94
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40
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Single molecule analysis reveals coexistence of stable serotonin transporter monomers and oligomers in the live cell plasma membrane.
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J Biol Chem
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2014
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0.94
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41
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A single glycine in extracellular loop 1 is the critical determinant for pharmacological specificity of dopamine D2 and D3 receptors.
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Mol Pharmacol
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2013
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0.92
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42
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Structure-Activity Relationships at the Monoamine Transporters for a Novel Series of Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide) Analogues.
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ACS Med Chem Lett
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2010
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0.91
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43
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Cocaine self-administration in dopamine D₃ receptor knockout mice.
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Exp Clin Psychopharmacol
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2012
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0.90
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44
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The dopamine D3 receptor antagonist NGB 2904 increases spontaneous and amphetamine-stimulated locomotion.
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Pharmacol Biochem Behav
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2007
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0.90
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45
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Dual probes for the dopamine transporter and sigma1 receptors: novel piperazinyl alkyl-bis(4'-fluorophenyl)amine analogues as potential cocaine-abuse therapeutic agents.
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J Med Chem
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2003
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0.89
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46
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Dopamine D3 receptor selective ligands with varying intrinsic efficacies at adenylyl cyclase inhibition and mitogenic signaling pathways.
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Synapse
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2010
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0.89
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47
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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.
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J Med Chem
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2003
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0.88
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48
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Structure-activity relationships at monoamine transporters for a series of N-substituted 3alpha-(bis[4-fluorophenyl]methoxy)tropanes: comparative molecular field analysis, synthesis, and pharmacological evaluation.
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J Med Chem
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2004
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0.88
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49
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Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D₃ receptor antagonists.
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J Med Chem
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2014
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0.88
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50
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The discriminative stimulus effects of dopamine D2- and D3-preferring agonists in rats.
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Psychopharmacology (Berl)
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2008
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0.88
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51
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Radioiodinated azide and isothiocyanate derivatives of cocaine for irreversible labeling of dopamine transporters: synthesis and covalent binding studies.
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Bioconjug Chem
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2005
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0.87
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52
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Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile) analogues at monoamine transporters.
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J Med Chem
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2010
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0.87
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53
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A rhodamine-labeled citalopram analogue as a high-affinity fluorescent probe for the serotonin transporter.
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Bioorg Med Chem Lett
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2012
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0.85
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54
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Relations between stimulation of mesolimbic dopamine and place conditioning in rats produced by cocaine or drugs that are tolerant to dopamine transporter conformational change.
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Psychopharmacology (Berl)
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2013
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0.85
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55
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Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.
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Bioorg Med Chem
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2010
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0.85
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56
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Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5.
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Bioorg Med Chem Lett
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2010
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0.84
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57
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Design and synthesis of 1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) analogues as novel probes for the serotonin transporter S1 and S2 binding sites.
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J Med Chem
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2013
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0.84
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58
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Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol.
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J Med Chem
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2008
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0.82
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59
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Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.
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ACS Med Chem Lett
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2012
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0.81
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60
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Fenobam sulfate inhibits cocaine-taking and cocaine-seeking behavior in rats: implications for addiction treatment in humans.
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Psychopharmacology (Berl)
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2013
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0.81
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61
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Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.
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J Med Chem
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2004
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0.81
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62
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A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats.
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Addict Biol
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2013
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0.81
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63
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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.
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J Med Chem
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2006
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0.81
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64
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Attenuation of the stimulant and convulsant effects of cocaine by 17-substituted-3-hydroxy and 3-alkoxy derivatives of dextromethorphan.
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Pharmacol Biochem Behav
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2003
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0.80
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65
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Three-dimensional quantitative structure-activity relationships of mazindol analogues at the dopamine transporter.
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J Med Chem
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2002
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0.80
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66
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Synthesis and monoamine transporter binding of 2-(diarylmethoxymethyl)-3 beta-aryltropane derivatives.
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J Med Chem
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2004
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0.80
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67
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Characterization of the transport, metabolism, and pharmacokinetics of the dopamine D3 receptor-selective fluorenyl- and 2-pyridylphenyl amides developed for treatment of psychostimulant abuse.
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J Pharmacol Exp Ther
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2010
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0.79
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68
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Dual DAT/sigma1 receptor ligands based on 3-(4-(3-(bis(4-fluorophenyl)amino)propyl)piperazin-1-yl)-1-phenylpropan-1-ol.
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Bioorg Med Chem Lett
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2008
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0.79
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69
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Applicability of the dopamine and rate hypotheses in explaining the differences in behavioral pharmacology of the chloro-benztropine analogs: studies conducted using intracerebral microdialysis and population pharmacodynamic modeling.
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J Pharmacol Exp Ther
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2007
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0.78
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70
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Enantioselective synthesis of S-(+)-2beta-carboalkoxy-3alpha-[bis(4-fluorophenyl)methoxy]tropanes as novel probes for the dopamine transporter.
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Bioorg Med Chem Lett
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2002
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0.78
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71
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Evaluation of the D3 dopamine receptor selective agonist/partial agonist PG01042 on L-dopa dependent animal involuntary movements in rats.
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Neuropharmacology
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2010
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0.78
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72
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The effect of 6-substituted-4',4"-difluorobenztropines on monoamine transporters and the muscarinic M1 receptor.
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Bioorg Med Chem Lett
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2004
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Elucidation of structural elements for selectivity across monoamine transporters: novel 2-[(diphenylmethyl)sulfinyl]acetamide (modafinil) analogues.
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J Med Chem
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2014
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74
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Novel Analogues of (R)-5-(Methylamino)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinolin-2(1H)-one (Sumanirole) Provide Clues to Dopamine D2/D3 Receptor Agonist Selectivity.
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J Med Chem
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2016
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75
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Comparative structure-activity relationships of benztropine analogues at the dopamine transporter and histamine H(1) receptors.
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Bioorg Med Chem
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2006
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0.76
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76
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Dopaminergic regulation of dopamine D3 and D3nf receptor mRNA expression.
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Synapse
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2010
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N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.
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Bioorg Med Chem Lett
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2005
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0.75
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