药物对神经肽及其受体的影响:在治疗慢性疼痛方面希望很大,但成效一般。

IF 4 3区 医学 Q1 PHARMACOLOGY & PHARMACY
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引用次数: 0

摘要

神经肽,包括速激肽、血管内皮生长因子和体生长抑素,定位于痛觉初级传入神经元的肽能亚群。速激肽和 CGRP 具有代痛觉作用,而体生长抑素则是一种抗痛觉介质。为开发速激肽和 CGRP 拮抗剂以及体生长抑素激动剂作为镇痛剂,人们进行了大量的药物研究。CGRP 受体拮抗剂是治疗偏头痛的有效且耐受性良好的药物。针对 CGRP 或其受体的单克隆抗体可用于偏头痛的预防性治疗。速激肽 NK1 受体拮抗剂镇痛效果不佳,但可用于化疗引起的恶心和呕吐。新型口服活性体生长抑素 4 受体激动剂是治疗各种疼痛病症的有希望的候选药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Drug effects on neuropeptides and their receptors: Big hopes but moderate success in the treatment of chronic pain

Neuropeptides, including tachykinins, CGRP, and somatostatin, are localized in a peptidergic subgroup of nociceptive primary afferent neurons. Tachykinins and CGRP are pronociceptive, somatostatin is an antinociceptive mediator. Intensive drug research has been performed to develop tachykinin and CGRP antagonists, and somatostatin agonists as analgesics. CGRP receptor antagonists are efficacious and well-tolerated drugs in migraine. Monoclonal antibodies against CGRP or its receptor are used for the prophylactic treatment of migraine. Tachykinin NK1 receptor antagonists failed as analgesics but are used for chemotherapy-induced nausea and vomiting. New, orally active somatostatin 4 receptor agonists are promising drug candidates for treating various pain conditions.

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来源期刊
CiteScore
8.80
自引率
2.50%
发文量
131
审稿时长
4-8 weeks
期刊介绍: Current Opinion in Pharmacology (COPHAR) publishes authoritative, comprehensive, and systematic reviews. COPHAR helps specialists keep up to date with a clear and readable synthesis on current advances in pharmacology and drug discovery. Expert authors annotate the most interesting papers from the expanding volume of information published today, saving valuable time and giving the reader insight on areas of importance.
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