241499-17-2
| 中文名稱 | 241499-17-2 |
|---|---|
| 中文同義詞 | 化合物 T12153;化合物 N-TYPE CALCIUM CHANNEL BLOCKER-1 |
| 英文名稱 | N-type calcium channel blocker-1 |
| 英文同義詞 | 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)-;N type calcium channel blocker 1,Ntype calcium channel blocker1 |
| CAS號 | 241499-17-2 |
| 分子式 | C31H47N3 |
| 分子量 | 461.73 |
| EINECS號 | |
| 相關(guān)類別 | |
| Mol文件 | 241499-17-2.mol |
| 結(jié)構(gòu)式 |  |
241499-17-2 性質(zhì)
| 沸點 | 569.9±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.013±0.06 g/cm3(Predicted) |
| 儲存條件 | Store at -20°C |
| 溶解度 | 溶于二甲基亞砜 |
| 酸度系數(shù)(pKa) | 8.89±0.10(Predicted) |
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).