TRPV1 binds TRPV1 blockers

Capsazepine is a synthetic antagonist of capsaicin. It is used as a biochemical tool in the study of TRPV ion channels (Valenzano & Sun 2004). Capsazepine blocks the painful sensation of heat caused by capsaicin which activates the TRPV1 ion channel (Bevan et al. 1992). Another potent TRPV1 channel blocker is ruthenium red, used as another tool for TRPV channel pharmacology (McIntyre et al. 2001, Smart et al. 2001). Antagonists of PRPV1 have yet to reach the clinic. While capsazepine has proven a useful tool for unraveling the molecular pharmacology of TRPV1, in vivo studies have had limited success due to poor pharmacokinetic properties and species selectivity (Valenzano & Sun 2004).

卡巴塞平是一种合成的辣椒素拮抗剂。它在研究 TRPV 离子通道（Valenzano & Sun 2004）的生物化学工具中得到了应用。卡巴塞平能够阻断由辣椒素激活的 TRPV1 离子通道所引起的痛觉热感（Bevan et al. 1992）。另一种高效的 TRPV1 通道阻断剂是钌红，它被用作 TRPV 通道药理学的另一项工具（McIntyre et al. 2001, Smart et al. 2001）。PRPV1 的拮抗剂尚未进入临床应用。尽管卡巴塞平已被证明是解析 TRPV1 分子药理学的一个有用工具，但由于其较差的药代动力学特性和物种选择性，体内研究仍取得了有限的成果（Valenzano & Sun 2004）。