241499-17-2

中文名称 241499-17-2

英文名称 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 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T12153

英文别名

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)-

物理化学性质

沸点569.9±50.0 °C(Predicted)

密度1.013±0.06 g/cm3(Predicted)

储存条件-20°C储存

溶解度溶于二甲基亚砜

酸度系数(pKa)8.89±0.10(Predicted)

常见问题列表

生物活性

N-type calcium channel blocker-1是有口服活性的麻醉剂，可阻断N型钙离子通道 (N-type calcium channels)，在IMR32试验中 IC50 值为0.7 μM。

靶点

IC50: 0.7 μM (N-type calcium channels)

体外研究

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.

体内研究

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).