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首页> 外文期刊>Expert opinion on pharmacotherapy >Mecamylamine - a nicotinic acetylcholine receptor antagonist with potential for the treatment of neuropsychiatric disorders.
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Mecamylamine - a nicotinic acetylcholine receptor antagonist with potential for the treatment of neuropsychiatric disorders.

机译：咪酰胺 - 一种烟碱乙酰胆碱受体拮抗剂，具有治疗神经精神疾病的潜力。

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摘要

Mecamylamine (Inversine), the first orally available antihypertensive agent launched in the 1950s, is rarely used today for hypertension because of its widespread ganglionic side effects at antihypertensive doses (25 - 90 mg/day). However, more recent clinical studies suggest that mecamylamine is effective at much lower doses for blocking the central and peripheral effects of nicotine. Pharmacologically, mecamylamine has been well characterized as a nonselective and noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). Because mecamylamine easily crosses the blood - brain barrier at relatively low doses (2.5 - 10 mg), it has been used by several research groups over the past two decades investigating the role of central nAChRs in the etiology and treatment of various neuropsychiatric disorders, including addiction disorders, Tourette's syndrome, schizophrenia and various cognitive and mood disorders. Two independent Phase II clinical trials recently confirmed mecamylamine's hypothesized antidepressant activity and suggest that it may be effective as an augmentation pharmacotherapy for SSRI treatment resistant major depression. These areas of investigation for mecamylamine are reviewed and recommendations for future research directions are proposed.
机译：MeCamylamine（Inversine），在20世纪50年代推出的第一个口服抗高血压剂，今天很少用于高血压，因为其在抗高血压剂量（25-90毫克/天）的广泛神经节副作用。然而，最近的临床研究表明，MeCamylamine在低得多剂量下有效，以阻断尼古丁的中央和周围效应。药理学上，咪酰胺精确地表征为烟碱乙酰胆碱受体（NACHRS）的非选择性和非竞争性拮抗剂。因为咪酰胺在相对较低剂量（2.5-10mg）中容易穿过血脑屏障，因此在过去的二十年中，几十年来，在过去的二十年中已经使用了中央NACHR在各种神经精神疾病的病因和治疗中的作用，包括成瘾障碍，Tourette的综合征，精神分裂症和各种认知和情绪障碍。两种独立的第II期临床试验最近证实了MeCamylamine的假设抗抑郁活性，并表明它可能是SSRI治疗抗性重大抑郁症的增强药物治疗。审查了这些对MeCamylamine的调查领域，并提出了未来的研究方向的建议。

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