Szallasi Arpad, Cortright Daniel N, Blum Charles A, Eid Samer R
Department of Pathology, Monmouth Medical Center, Long Branch, New Jersey 07740, USA.
Nat Rev Drug Discov. 2007 May;6(5):357-72. doi: 10.1038/nrd2280.
The clinical use of TRPV1 (transient receptor potential vanilloid subfamily, member 1; also known as VR1) antagonists is based on the concept that endogenous agonists acting on TRPV1 might provide a major contribution to certain pain conditions. Indeed, a number of small-molecule TRPV1 antagonists are already undergoing Phase I/II clinical trials for the indications of chronic inflammatory pain and migraine. Moreover, animal models suggest a therapeutic value for TRPV1 antagonists in the treatment of other types of pain, including pain from cancer. We argue that TRPV1 antagonists alone or in conjunction with other analgesics will improve the quality of life of people with migraine, chronic intractable pain secondary to cancer, AIDS or diabetes. Moreover, emerging data indicate that TRPV1 antagonists could also be useful in treating disorders other than pain, such as urinary urge incontinence, chronic cough and irritable bowel syndrome. The lack of effective drugs for treating many of these conditions highlights the need for further investigation into the therapeutic potential of TRPV1 antagonists.
瞬时受体电位香草酸亚家族成员1（TRPV1，也称为VR1）拮抗剂的临床应用基于这样一种概念，即作用于TRPV1的内源性激动剂可能在某些疼痛状况中起主要作用。事实上，一些小分子TRPV1拮抗剂已在针对慢性炎性疼痛和偏头痛适应症进行I/II期临床试验。此外，动物模型表明TRPV1拮抗剂在治疗其他类型的疼痛（包括癌症疼痛）方面具有治疗价值。我们认为，TRPV1拮抗剂单独使用或与其他镇痛药联合使用将改善偏头痛患者、继发于癌症、艾滋病或糖尿病的慢性顽固性疼痛患者的生活质量。此外，新出现的数据表明，TRPV1拮抗剂在治疗除疼痛以外的其他疾病（如急迫性尿失禁、慢性咳嗽和肠易激综合征）方面也可能有用。治疗许多这些疾病缺乏有效药物凸显了进一步研究TRPV1拮抗剂治疗潜力的必要性。
