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123388-25-0

中文名稱 123388-25-0
英文名稱 Semotiadil (recemate fumarate)
CAS 123388-25-0
分子式 C33H36N2O10S
分子量 652.711
MOL 文件 123388-25-0.mol
123388-25-0 結(jié)構(gòu)式 123388-25-0 結(jié)構(gòu)式

基本信息

中文別名
司莫地爾 (準(zhǔn)外消旋體富馬酸鹽)
英文別名
Semotiadil (recemate fumarate)

物理化學(xué)性質(zhì)

熔點131-133 °C(Solv: ethanol (64-17-5))
儲存條件-20°C儲存
溶解度溶于二甲基亞砜

常見問題列表

生物活性
Semotiadil recemate fumarate 是 Semotiadil fumarate 的外消旋體。Semotiadil fumarate 是一種新型的血管選擇性的 Ca2+ 通道拮抗劑。
靶點

Ca 2+ channel

體外研究

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 (IC 50 =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.

體內(nèi)研究

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.

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