大麻素 CB1 受体的正性异位调节剂能否安全有效地治疗慢性疼痛？

IF 4 3区医学 Q1 PHARMACOLOGY & PHARMACY

Current Opinion in Pharmacology Pub Date : 2024-10-23 DOI:10.1016/j.coph.2024.102495

Hayley M. Green , Michelle Glass

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引用次数: 0

摘要

大麻素是一种有效的镇痛剂，但会产生大麻拟效作用和耐受性。大麻素 CB1 受体（CB1）的异构配体可以利用大麻素的镇痛效果，同时减少不良反应。CB1 异构配体的结合位点在地形上不同于正构结合位点。CB1 异构配体已被证明是有效的镇痛药物，似乎不会产生不良反应或耐受性。虽然这种治疗特征表明 CB1 异构配体可以有效治疗慢性疼痛，但其分子作用机制仍不清楚。

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Could positive allosteric modulators of the cannabinoid CB1 receptor be efficacious and safe for the treatment of chronic pain?

Cannabinoids are effective analgesics but induce adverse cannabimimetic effects and the development of tolerance. Allosteric ligands of the cannabinoid CB₁ receptor (CB₁) may harness the pain-relieving effects of cannabinoids with reduced adverse effects. CB₁ allosteric ligands bind at a site topographically distinct from the orthosteric binding site. CB₁ allosteric ligands have been shown to be effective pain-relieving drugs that do not appear to result in the production of adverse effects or the development of tolerance. While this therapeutic profile indicates that CB₁ allosteric ligands could be an effective treatment for chronic pain, their molecular mechanism of action remains unclear.

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来源期刊

Current Opinion in Pharmacology 医学-药学

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.