Ally A I, Horrobin D F, Manku M S, Morgan R O, Karmazyn M, Karmali R A, Cunnane S C
Can J Physiol Pharmacol. 1978 Jun;56(3):520-3. doi: 10.1139/y78-080.
Dantrolene sodium has been shown to block the release of intracellular calcium in skeletal muscle. It has been proposed that dantrolene blocks the movement and (or) action of a natural calcium ionophore. In a rat vascular preparation dantrolene was found to inhibit pressor responses to noradrenaline and angiotensin but not those to potassium with an IC50 concentration within the therapeutic levels in man. Imidazole, an inhibitor of thromboxane A2 (TXA2) synthesis, had similar actions to dantrolene. Interactions between imidazole and dantrolene suggested that dantrolene may be a competitive antagonist of TXA2 in muscle. We report the first demonstration of an effect of dantrolene sodium on smooth muscle contractility and suggest that TXA2 is an essential modulator of vascular reactivity. A similar role has been shown for TXA2 in platelets.
已证实丹曲林钠可阻断骨骼肌细胞内钙的释放。有人提出，丹曲林可阻断天然钙离子载体的移动和（或）作用。在大鼠血管制剂中，发现丹曲林可抑制对去甲肾上腺素和血管紧张素的升压反应，但对钾的升压反应无抑制作用，其半数抑制浓度（IC50）在人体治疗水平范围内。血栓素A2（TXA2）合成抑制剂咪唑与丹曲林有相似作用。咪唑与丹曲林之间的相互作用表明，丹曲林可能是肌肉中TXA2的竞争性拮抗剂。我们首次证明了丹曲林钠对平滑肌收缩性的影响，并表明TXA2是血管反应性的重要调节因子。TXA2在血小板中也发挥了类似作用。
