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241499-17-2

中文名稱 241499-17-2
英文名稱 N-type calcium channel blocker-1
CAS 241499-17-2
分子式 C31H47N3
分子量 461.73
MOL 文件 241499-17-2.mol
241499-17-2 結(jié)構(gòu)式 241499-17-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12153
英文別名
N-type calcium channel blocker-1
4-Piperidinamine, 1-[[4-(dimethylamino)phenyl]methyl]-N-[4-(3,3-dimethylbutyl)phenyl]-N-(3-methyl-2-buten-1-yl)-

物理化學(xué)性質(zhì)

沸點(diǎn)569.9±50.0 °C(Predicted)
密度1.013±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)8.89±0.10(Predicted)

常見問題列表

生物活性
N-type calcium channel blocker-1是有口服活性的麻醉劑,可阻斷N型鈣離子通道 (N-type calcium channels),在IMR32試驗(yàn)中 IC50 值為0.7 μM。
靶點(diǎn)

IC50: 0.7 μM (N-type calcium channels)

體外研究

N-type calcium channel blocker-1 shows good activities in the IMR32 assay (IC 50 =0.7 μM). N-type calcium channel blocker-1 is the most orally active N-type calcium channel blocker for analgesia found in a series of compounds.

體內(nèi)研究

N-type calcium channel blocker-1 shows good activities in the acetic acid anti-writhing model (ED 50 =4 mg/kg, iv). N-type calcium channel blocker-1 exhibits oral activity (ED 50 =12 mg/kg, po). A time course study of N-type calcium channel blocker-1 in the anti-writhing model indicates that the CF-1 mice have maximal effect at 120 min after oral dosing at 60 mg/kg. Further evaluation of N-type calcium channel blocker-1 demonstrates several important and advantageous features: the pharmacokinetic profile of N-type calcium channel blocker-1 is improved (Versus of 5.9 L/kg and CL of 26 mL/min/kg) and the logPn of 26 is favorable for CNS agent (logPn measured to be 3.20).

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