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Review of the pharmacological and clinical profile of rimcazole.

机译：rimcazole的药理和临床概况综述。

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摘要

Rimcazole is a carbazole derivative that acts in part as a sigma receptor antagonist. Wellcome Research Laboratories introduced this compound during the 1980s when it was hypothesized to be a novel antipsychotic with an improved side effect profile. However, subsequent clinical trials demonstrated that rimcazole lacked efficacy in schizophrenic patients and it is now primarily used as an experimental tool. In addition to its actions as a sigma receptor antagonist, rimcazole also has high affinity for dopamine transporters, and in recent years it has served as a lead compound for the development of novel dopamine transporter ligands. Although rimcazole cannot be considered a selective ligand for sigma receptors, the recent development of other selective agonists and antagonists for sigma receptors have aided in clarifying the involvement of these receptors in the actions of rimcazole. Many of the physiological and behavioral effects of rimcazole can in fact be ascribed to its action as a sigma receptor antagonist, although there are exceptions. Rimcazole is likely to have a continued role in elucidating sigma receptor function in either in vitro or in vivo systems where sigma receptor-mediated effects can be studied independently of the influence of dopamine and serotonin transporters.
机译：Rimcazole是咔唑衍生物，部分充当sigma受体拮抗剂。威康研究实验室（Wellcome Research Laboratories）于1980年代引入了该化合物，当时该化合物被认为是具有改善的副作用特征的新型抗精神病药。但是，随后的临床试验表明，rimcazole在精神分裂症患者中缺乏疗效，现在主要用作实验工具。 rimcazole除了作为sigma受体拮抗剂的作用外，还对多巴胺转运蛋白具有很高的亲和力，近年来，它已成为开发新型多巴胺转运蛋白配体的先导化合物。尽管不能将rimcazole视为sigma受体的选择性配体，但sigma受体的其他选择性激动剂和拮抗剂的最新发展有助于阐明这些受体在rimcazole的作用中的作用。实际上，rimcazole的许多生理和行为影响都可以归因于它作为sigma受体拮抗剂的作用，尽管有例外。在体外或体内系统中，Rimcazole可能在阐明sigma受体功能方面继续发挥作用，在该系统中，可以独立于多巴胺和血清素转运蛋白的影响而研究sigma受体介导的作用。

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