Mittelstadt Scott W, Nelson Richard A, Daanen Jerome F, King Andrew J, Kort Michael E, Kym Philip R, Lubbers Nathan L, Cox Bryan F, Lynch James J
Department of Integrative Pharmacology, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064-6118, USA.
Blood Coagul Fibrinolysis. 2012 Jan;23(1):94-7. doi: 10.1097/MBC.0b013e32834ddf18.
Capsaicin is an agonist of transient receptor potential vanilloid type 1 (TRPV1), in which it can act as a neuronal stimulant and result in nociception. Capsaicin also affects a variety of nonneuronal tissues, in which its mechanisms of action are less certain. The present study investigated whether the inhibitory effects of capsaicin on platelet aggregation are mediated via TRPV1. Venous whole blood obtained from beagle dogs (n = 6) was preincubated with capsaicin and/or the potent and selective competitive TRPV1 antagonist, A-993610 and then exposed to collagen (2 μg/ml). An aggregometer was used to quantify the platelet response. Capsaicin exposure inhibited collagen-induced platelet aggregation in a concentration-dependent manner, with significant effects at 10 and 30 μg capsaicin per millilitre. A-993610 alone (0.1-1.0 μg/ml) had no effects on collagen-induced platelet aggregation, nor did it have any effects on capsaicin's ability to inhibit platelet aggregation. The current results agree with previous findings that capsaicin can inhibit platelet aggregation. In addition, the present study demonstrates that capsaicin's inhibitory effect on collagen-induced canine platelet aggregation is not mediated by TRPV1.
辣椒素是瞬时受体电位香草酸亚型1(TRPV1)的激动剂,在其中它可作为一种神经元刺激物并导致伤害感受。辣椒素还会影响多种非神经组织,其作用机制尚不太明确。本研究调查了辣椒素对血小板聚集的抑制作用是否通过TRPV1介导。从比格犬(n = 6)采集的静脉全血先与辣椒素和/或强效选择性竞争性TRPV1拮抗剂A-993610预孵育,然后暴露于胶原蛋白(2μg/ml)。使用血小板聚集仪定量血小板反应。暴露于辣椒素以浓度依赖性方式抑制胶原蛋白诱导的血小板聚集,每毫升10和30μg辣椒素时具有显著作用。单独使用A-993610(0.1 - 1.0μg/ml)对胶原蛋白诱导的血小板聚集没有影响,对辣椒素抑制血小板聚集的能力也没有任何影响。目前的结果与之前关于辣椒素可抑制血小板聚集的发现一致。此外,本研究表明辣椒素对胶原蛋白诱导的犬血小板聚集的抑制作用不是由TRPV1介导的。