索玛的滥用潜力:以 GABA(A)受体为目标。

Molecular and cellular pharmacology Pub Date : 2009-01-01
Lorie A Gonzalez, Michael B Gatch, Michael J Forster, Glenn H Dillon
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引用次数: 0

摘要

索玛(Soma(®))(carisoprodol)是一种滥用现象日益严重的中枢作用型肌肉松弛剂。尽管滥用 carisoprodol 的现象很普遍,但其作用机制仍不清楚。它的镇静作用通常归因于其主要代谢物甲丙氨酯对 GABA(A)受体(GABA(A)R)的作用,这也是其治疗和娱乐用途的原因。甲丙氨酯是联邦一级的管制物质;具有讽刺意味的是,目前卡里索并没有被归类为管制物质。最近,我们利用行为学和分子药理学方法证明,卡里索本身能够以类似于中枢神经系统抑制剂的方式调节 GABA(A)R 的功能。它与这类药物在功能上的相似性极易使人上瘾,这可能是卡里索布洛具有滥用潜力的原因之一。卡里索普多的作用位点尚未确定;根据我们的研究,与苯二氮杂卓或巴比妥类药物作用位点发生相互作用的可能性不大。最近的这些发现,再加上文献中的大量报道,支持了应重新评估卡里索布洛醇不受管制地位的论点。
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Abuse Potential of Soma: the GABA(A) Receptor as a Target.

Soma(®) (carisoprodol) is an increasingly abused, centrally-acting muscle relaxant. Despite the prevalence of carisoprodol abuse, its mechanism of action remains unclear. Its sedative effects, which contribute to its therapeutic and recreational use, are generally attributed to the actions of its primary metabolite, meprobamate, at GABA(A) receptors (GABA(A)R). Meprobamate is a controlled substance at the federal level; ironically, carisoprodol is not currently classified as such. Using behavioral and molecular pharmacological approaches, we recently demonstrated carisoprodol, itself, is capable of modulating GABA(A)R function in a manner similar to central nervous system depressants. Its functional similarities with this highly addictive class of drugs may contribute to the abuse potential of carisoprodol. The site of action of carisoprodol has not been identified; based on our studies, interaction with benzodiazepine or barbiturate sites is unlikely. These recent findings, when coupled with numerous reports in the literature, support the contention that the non-controlled status of carisoprodol should be reevaluated.

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