Szallasi Arpad
Department of Pathology, Monmouth Medical Center, Long Branch, NJ 07740, USA.
Trends Pharmacol Sci. 2005 Sep;26(9):437-9. doi: 10.1016/j.tips.2005.07.001.
Studies with animals that are deficient in the vanilloid (capsaicin) receptor TRPV1 have confirmed the pivotal role that TRPV1 has in the development of post-inflammatory hyperalgesia, and enhanced TRPV1 expression has been described in various human disorders. Natural products have provided several lead structures for the development of vanilloid ligands. A recent study shows that piperine, the irritant principle in black pepper, is more efficient than capsaicin in the desensitization of human TRPV1, which suggests that this pharmacological aspect of vanilloids can be dissociated from its potency. This finding raises the intriguing possibility that piperine can be used as a chemical template for the design of improved TRPV1 agonists.
对缺乏香草酸(辣椒素)受体TRPV1的动物进行的研究证实了TRPV1在炎症后痛觉过敏发展中的关键作用,并且在各种人类疾病中都有TRPV1表达增强的描述。天然产物为香草酸配体的开发提供了几种先导结构。最近一项研究表明,黑胡椒中的刺激性成分胡椒碱在使人类TRPV1脱敏方面比辣椒素更有效,这表明香草酸的这一药理学特性可以与其效力相分离。这一发现引发了一个有趣的可能性,即胡椒碱可作为设计改良型TRPV1激动剂的化学模板。