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Corticotropin-releasing factor type-1 receptor antagonists: The next class of antidepressants?

机译:促肾上腺皮质激素释放因子1型受体拮抗剂:下一类抗抑郁药?

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摘要

Corticotropin-releasing factor (CRF) is a neuropeptide that plays a primary role in the neuroendocrine, autonomic, and behavioral responses to stressors. Numerous reports suggest that alterations in CRF function contribute to the pathogenesis of depression. Recently, selective nonpeptide CRF type 1 (CRF1) receptor antagonists have been discovered and several of these CRF1 receptor antagonists have demonstrated antidepressantlike efficacy in animals. The CRF1 receptor antagonists appear to be unique, as they exhibit antidepressant-like activity principally in animal models that are hyperresponsive to stress or under experimental conditions that alter endogenous stress-hormone activity. A nonpeptide CRF1 receptor antagonist has also been shown to reduce symptoms of major depression in an open-label clinical trial. Accumulating evidence supports a role for nonpeptide CRF1 receptor antagonists among the future pharmacotherapies for the treatment of depression. (c) 2005 Elsevier Inc. All rights reserved.
机译:促肾上腺皮质激素释放因子(CRF)是一种神经肽,在对应激源的神经内分泌,自主神经和行为反应中起主要作用。大量报告表明,CRF功能的改变与抑郁症的发病机理有关。最近,发现了选择性非肽1型CRF(CRF1)受体拮抗剂,这些CRF1受体拮抗剂中的几种已在动物中表现出抗抑郁样功效。 CRF1受体拮抗剂似乎是独特的,因为它们主要在对应激反应过度的动物模型中或在改变内源性应激激素活性的实验条件下表现出抗抑郁样活性。在开放标签的临床试验中,非肽CRF1受体拮抗剂还被证明可以减轻严重抑郁的症状。越来越多的证据支持在未来的抑郁症药物治疗中非肽CRF1受体拮抗剂的作用。 (c)2005 Elsevier Inc.保留所有权利。

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