title: New, potent cocaine analogs: ligand binding and transport studies in rat striatum.
abstract: Two potent cocaine analogs have been developed that have the highest known affinities for the cocaine binding site in rat striatum. Both 3 beta-(4-chlorophenyl)- (RTI-COC-31) and 3 beta-(4-methylphenyl)-tropane-2-carboxylic acid methyl ester (RTI-COC-32) compete for [3H]WIN 35,428 and [3H]mazindol binding with a IC50 that is 100 times more potent than that of (-) cocaine. Additionally, these compounds inhibit [3H]dopamine uptake with a similar, high potency. These results may lead to the development of high affinity probes for the cocaine binding site.
authors.affiliation: Neuroscience Branch, Addiction Research Center, National Institute on Drug Abuse, Baltimore, MD 21224.
authors.forename: J W
authors.initials: JW
authors.lastname: Boja
authors.forename: F I
authors.initials: FI
authors.lastname: Carroll
authors.forename: M A
authors.initials: MA
authors.lastname: Rahman
authors.forename: A
authors.initials: A
authors.lastname: Philip
authors.forename: A H
authors.initials: AH
authors.lastname: Lewin
authors.forename: M J
authors.initials: MJ
authors.lastname: Kuhar
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D001692:Biological Transport; D003042:Cocaine / Q000031:analogs & derivatives* / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism*; D004298:Dopamine / Q000378:metabolism; D066298:In Vitro Techniques; D011869:Radioligand Assay; D051381:Rats; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism
chemical_list: C067731:3-(4-chlorophenyl)tropane-2-carboxylic acid methyl ester; C067730:RTI-COC 32; C021279:(1R-(exo,exo))-3-(4-fluorophenyl)-8-methyl-8- azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester; C021278:troparil; D003042:Cocaine; D004298:Dopamine