Bross T E, Prescott S M, Majerus P W
Biochem Biophys Res Commun. 1983 Oct 14;116(1):68-74. doi: 10.1016/0006-291x(83)90381-9.
RHC 80267 inhibits diglyceride lipase activity in microsomes from canine platelets (1). Chau and Tai (2) reported that RHC 80267 prevents the transient accumulation of monoglyceride in thrombin-stimulated human platelets, while leaving arachidonate release unimpaired. In contrast, we find that while the drug inhibits both diglyceride lipase (I50 = 15 microM) and monoglyceride lipase (I50 = 11 microM) activities in platelet microsomes, it is ineffective when added to intact platelets. The transient intermediates in the diglyceride lipase pathway, 1,2-diglyceride and 2-monoglyceride, both accumulated after thrombin stimulation of intact platelets treated with RHC 80267, and arachidonate release was not inhibited. We conclude that RHC 80267 cannot be used to evaluate the diglyceride lipase pathway in intact platelets.
RHC 80267可抑制犬血小板微粒体中的甘油二酯脂肪酶活性(1)。Chau和Tai(2)报道，RHC 80267可防止凝血酶刺激的人血小板中甘油单酯的短暂积累，同时不影响花生四烯酸的释放。相比之下，我们发现，虽然该药物可抑制血小板微粒体中的甘油二酯脂肪酶(I50 = 15 microM)和甘油单酯脂肪酶(I50 = 11 microM)活性，但添加到完整血小板中时却无效。在用RHC 80267处理的完整血小板经凝血酶刺激后，甘油二酯脂肪酶途径中的瞬时中间体1,2-甘油二酯和2-甘油单酯均会积累，且花生四烯酸的释放未受抑制。我们得出结论，RHC 80267不能用于评估完整血小板中的甘油二酯脂肪酶途径。
