Glass F, Lippton H, Kadowitz P J
Prostaglandins Med. 1980 Aug;5(2):85-92. doi: 10.1016/0161-4630(80)90095-6.
The effects of several local anesthetics and propranolol, a beta receptor antagonist with local anesthetic activity, on adenosine 5'-diphosphate (ADP) and arachidonic acid (AA)-induced aggregation were studied in rabbit platelets. Platelet-rich plasma (PRP) was obtained from rabbits anesthetized with pentobarbital and changes in turbidity of PRP were measured with an aggregometer. Inhibition of platelet aggregation by the local anesthetics was expressed as the percent change in rate of aggregation from control value. Dibucaine was the most potent inhibitor of both AA- and ADP-induced aggregation. This inhibition was sensitive to external calcium concentration. In terms of potency dibucane > tetracine > lidocaine in inhibiting AA- and ADP-induced aggregation. Procaine was more effective against AA- than ADP-induced aggregation. Propanolol was comparable to the more potent local anesthetics. These data show that local anesthetics and propranolol inhibit both AA- and ADP-induced platelet aggregation and suggest that the mechanism of action is non-specific in nature.
研究了几种局部麻醉药以及具有局部麻醉活性的β受体拮抗剂普萘洛尔对兔血小板中5'-二磷酸腺苷(ADP)和花生四烯酸(AA)诱导的聚集的影响。从用戊巴比妥麻醉的兔子中获取富含血小板的血浆(PRP),并用聚集仪测量PRP的浊度变化。局部麻醉药对血小板聚集的抑制作用以聚集速率相对于对照值的变化百分比表示。丁卡因是AA和ADP诱导聚集的最有效抑制剂。这种抑制作用对细胞外钙浓度敏感。就抑制AA和ADP诱导的聚集的效力而言,丁卡因>丁哌卡因>利多卡因。普鲁卡因对AA诱导的聚集比对ADP诱导的聚集更有效。普萘洛尔与更有效的局部麻醉药相当。这些数据表明,局部麻醉药和普萘洛尔均可抑制AA和ADP诱导的血小板聚集,并表明其作用机制本质上是非特异性的。