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蛋白酶活化受体4(PAR4)是G蛋白偶联受体家族成员之一,可被凝血酶、胰蛋白酶活化。PAR4是血小板活化和炎症的强力调节受体,活化的PAR4可作为潜在的内源性镇痛因子,在正常和炎症条件下参与调节外周疼痛反应。PAR4通过致敏TRPV1、细胞内Ca2+的释放和刺激周围感觉神经末梢释放P物质和CGRP参与了炎症和疼痛的周围机制。PAR4直接与电压门控Ca2+通道的相互作用可能是PAR4对细胞除极诱发的Ca2+信号产生抑制作用和PAR4参与镇痛的作用机制。
Protease-activated receptor 4 (PAR4), a member of the G-protein coupled receptor family, is activated by thrombin and trypsin. PAR4 is a potent regulatory receptor for platelet activation and inflammation, and activated PAR4 may serve as a potential endogenous analgesic factor involved in regulating peripheral pain responses under normal and inflammatory conditions. PAR4 participates in the mechanisms of inflammation and pain by sensitizing TRPV1, releasing intracellular Ca2 +, and stimulating the release of substance P and CGRP from peripheral sensory nerve endings. The direct interaction of PAR4 with voltage-gated Ca2 + channels may be the mechanism by which PAR4 inhibits the depolarization-induced Ca2 + signal and PAR4 participates in analgesia.