Enouf J, Lévy-Toledano S
Br J Pharmacol. 1984 Mar;81(3):509-18. doi: 10.1111/j.1476-5381.1984.tb10104.x.
Phenothiazine analogues have been tested for their effect on calcium uptake into platelet membrane vesicles and on ionophore-induced platelet activation, both phenomena being Ca2+-dependent. Both calcium uptake into membrane vesicles and ionophore-induced platelet activation were inhibited by the drugs. Evidence for two inhibitors as potent as chlorpromazine and trifluoperazine was found. These drugs are apparently competitive inhibitors of calcium uptake. A structure-activity relationship has been established. The data suggest that the phenothiazines are able to inhibit calmodulin-insensitive calcium uptake of platelet membrane vesicles and that therefore they cannot be assumed to be selective inhibitors of calmodulin interactions under all circumstances.
已对吩噻嗪类似物对血小板膜囊泡钙摄取以及离子载体诱导的血小板活化的影响进行了测试，这两种现象均依赖于Ca2+。药物抑制了膜囊泡的钙摄取以及离子载体诱导的血小板活化。发现了两种与氯丙嗪和三氟拉嗪一样有效的抑制剂。这些药物显然是钙摄取的竞争性抑制剂。已建立了构效关系。数据表明，吩噻嗪能够抑制血小板膜囊泡对钙调蛋白不敏感的钙摄取，因此不能认为它们在所有情况下都是钙调蛋白相互作用的选择性抑制剂。
