Semotiadil recemate司莫地尔 (准外消旋体

富马酸盐),123388-25-0

价格询价

品牌MedChemExpress(MCE)
产地美国
货号HY-U00026
更新日期2025年12月05日

MedChemExpress LLC

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Semotiadil recemate fumarate

CAS No. : 123388-25-0

MCE 国际站：Semotiadil recemate fumarate

产品活性：Semotiadil recemate fumarate 是 Semotiadil fumarate 的外消旋体。Semotiadil fumarate 是一种新型的血管选择性的 Ca²⁺ 通道拮抗剂。

研究领域：Membrane Transporter/Ion Channel | Neuronal Signaling

作用靶点：Calcium Channel

In Vitro: Semotiadil in a concentration of 1 μM produces an inhibition of 12.4±9.7% and in a concentration of 10 μM an inhibition of 25±11.0%. Effects of Semotiadil on the voltage-dependent Ca current (ICa) are investigated in dispersed smooth muscle cells of the rabbit portal vein. At a holding potential of -100 mV, Semotiadil (> or =0.1 μM; dissolved in DMSO) inhibits the ICa in a concentration-dependent manner (IC₅₀=2.0 μM). At a holding potential of -80 mV or -60 mV, the concentration-inhibition curve observed in the presence of Semotiadil is shifted to the left compared with that observed at -100 mV; and Semotiadil shifts the voltage-dependent inactivation curve to the left. The curve for the decay of ICa is fitted with two time constants. Semotiadil (<1 μM) reduces the slow but not the fast time constant. The curve for the recovery from ICa inactivation also consisted of two time constants, and Semotiadil (1 microM) prolongs the slow recovery. Semotiadil dissolved in deionized water more potently inhibits ICa than Semotiadil dissolved in DMSO.

In Vivo: Semotiadil fumarate, a novel benzothiazine calcium antagonist, is given alone or in combination with either Enalapril or trichlormethiazide to conscious, spontaneously hypertensive, rats daily for 2 weeks. When given alone, the antihypertensive effects of Semotiadil (10 mg/kg, p.o.) and Enalapril (5 mg/kg, p.o.) first became apparent after the 3rd dose and thereafter the effects appeared to develop daily although this effect had waned by the time of the next dose. These results indicate that combined daily dosing of Semotiadil, especially with Enalapril, each at relatively low doses may be able to control hypertension in a continuous manner.