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新型强效可卡因类似物：大鼠纹状体中的配体结合与转运研究

New, potent cocaine analogs: ligand binding and transport studies in rat striatum.

作者信息

Boja J W, Carroll F I, Rahman M A, Philip A, Lewin A H, Kuhar M J

机构信息

Neuroscience Branch, Addiction Research Center, National Institute on Drug Abuse, Baltimore, MD 21224.

出版信息

Eur J Pharmacol. 1990 Aug 10;184(2-3):329-32. doi: 10.1016/0014-2999(90)90627-i.

DOI:10.1016/0014-2999(90)90627-i
PMID:2079102
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.

摘要

已经开发出两种强效可卡因类似物，它们对大鼠纹状体中可卡因结合位点具有已知的最高亲和力。3β-(4-氯苯基)-（RTI-COC-31）和3β-(4-甲基苯基)-托烷-2-羧酸甲酯（RTI-COC-32）都能与[3H]WIN 35,428和[3H]吗茚酮竞争结合，其IC50比（-）可卡因强100倍。此外，这些化合物以相似的高效力抑制[3H]多巴胺摄取。这些结果可能会导致开发出针对可卡因结合位点的高亲和力探针。

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