Meltzer P C, Liang A Y, Brownell A L, Elmaleh D R, Madras B K
Organix Inc., Woburn, Massachusetts 01801.
J Med Chem. 1993 Apr 2;36(7):855-62. doi: 10.1021/jm00059a010.
It is now accepted that (-)-cocaine binds to specific recognition sites associated with monoamine transporters in the mammalian brain. In this study, several analogs of 3 beta-phenyltropane-2 beta-carboxylic acid methyl ester were prepared and their potency for inhibiting the binding of [3H]-3 beta-(4-fluorophenyl)tropane-2 beta-carboxylic acid methyl ester to primate caudate-putamen was evaluated. The synthesis and binding affinity of 3 beta-(3,4- dichlorophenyl)tropane-2 beta-carboxylic acid methyl ester, one of the most potent cocaine congeners yet reported, is presented. The feasibility of synthesizing high-affinity ligands for cocaine recognition sites and their suitability as PET imaging ligands for cocaine receptors in vivo is demonstrated.
现在人们已经接受，（-）-可卡因与哺乳动物脑中与单胺转运体相关的特定识别位点结合。在本研究中，制备了几种3β-苯基托烷-2β-羧酸甲酯类似物，并评估了它们抑制[3H]-3β-（4-氟苯基）托烷-2β-羧酸甲酯与灵长类动物尾状核-壳核结合的效力。本文介绍了3β-（3,4-二氯苯基）托烷-2β-羧酸甲酯的合成及其结合亲和力，它是迄今报道的最有效的可卡因同系物之一。本文还证明了合成可卡因识别位点高亲和力配体的可行性及其作为体内可卡因受体PET成像配体的适用性。
