Izenwasser S, Newman A H, Katz J L
Psychobiology Section, NIDA Addiction Research Center, Baltimore, MD 21224.
Eur J Pharmacol. 1993 Oct 19;243(2):201-5. doi: 10.1016/0014-2999(93)90381-q.
Cocaine and several sigma receptor ligands inhibit dopamine uptake via a common site. This is evidenced by a concentration-dependent inhibition of dopamine uptake and displacement of the binding of [3H]WIN 35,428 (also called CFT), a cocaine analog with high affinity for the dopamine transporter. Since several sigma receptor ligands have been shown to block the stimulant effects of cocaine, this site may serve as a target for future drug development to treat cocaine abuse.
可卡因和几种西格玛受体配体通过一个共同位点抑制多巴胺摄取。这一点通过对多巴胺摄取的浓度依赖性抑制以及对[3H]WIN 35,428(也称为CFT,一种对多巴胺转运体具有高亲和力的可卡因类似物)结合的置换得到证明。由于已经表明几种西格玛受体配体可阻断可卡因的兴奋作用,该位点可能成为未来治疗可卡因滥用药物开发的靶点。