241499-17-2
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- CAS号:
- 241499-17-2
- 英文名:
- N-type calcium channel blocker-1
- 英文别名:
- N-type calcium channel blocker-1;N type calcium channel blocker 1,Ntype calcium channel blocker1;4-Piperidinamine, 1-[[4-(dimethylamino)phenyl]methyl]-N-[4-(3,3-dimethylbutyl)phenyl]-N-(3-methyl-2-buten-1-yl)-
- 中文名:
- 241499-17-2
- 中文别名:
- 化合物 T12153
- CBNumber:
- CB44797087
- 分子式:
- C31H47N3
- 分子量:
- 461.73
- MOL File:
- 241499-17-2.mol
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241499-17-2化学性质
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沸点:
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569.9±50.0 °C(Predicted)
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密度:
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1.013±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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8.89±0.10(Predicted)
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241499-17-2性质、用途与生产工艺
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。
IC50: 0.7 μM (N-type calcium channels)
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.
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).
241499-17-2
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241499-17-2, 241499-17-2 相关搜索:
- C31H47N3
- 化合物 T12153
- 241499-17-2
- N type calcium channel blocker 1,Ntype calcium channel blocker1
- 4-Piperidinamine, 1-[[4-(dimethylamino)phenyl]methyl]-N-[4-(3,3-dimethylbutyl)phenyl]-N-(3-methyl-2-buten-1-yl)-
- N-type calcium channel blocker-1