(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE
生物活性靶点体外研究体内研究 用途与合成方法 MSDS (1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE价格(试剂级) 上下游产品信息
| 中文名称 | (1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE |
|---|---|
| 中文同义词 | 化合物 T16556;化合物 PNU-142633 |
| 英文名称 | (1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE |
| 英文同义词 | (1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE;PNU 142633;PNU142633,PNU 142633;1H-2-Benzopyran-6-carboxamide, 1-[2-[4-[4-(aminocarbonyl)phenyl]-1-piperazinyl]ethyl]-3,4-dihydro-N-methyl-, (1S)- |
| CAS号 | 187665-65-2 |
| 分子式 | C24H30N4O3 |
| 分子量 | 422.52 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 187665-65-2.mol |
| 结构式 | ![(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE 结构式](CAS/GIF/187665-65-2.gif) |
(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE 性质
| 沸点 | 652.5±55.0 °C(Predicted) |
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| 密度 | 1?+-.0.06 g/cm3(Predicted) |
| 储存条件 | Store at +4°C |
| 溶解度 | 在 DMSO 中溶解度为 100 mM |
| 形态 | 粉末 |
| 酸度系数(pKa) | 15.27±0.40(Predicted) |
| 颜色 | 白色至米白色 |
(1S)-1-[2-[4-[4-(AMINOCARBONYL)PHENYL]-1-PIPERAZINYL]ETHYL]-3,4-DIHYDRO-N-METHYL-1H-2-BENZOPYRAN-6-CARBOXAMIDE 用途与合成方法
PNU-142633 是一种高亲和力，选择性和口服活性的 5-HT1D 激动剂，对人 5-HT1D 受体和人 5-HT1B 受体的 Ki 分别为 6 nM 和 >18 000 nM。PNU-142633 具有抗偏头痛功效。
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5-HT 1D Receptor 6 nM (Ki) |
The intrinsic activity of PNU-142633 at the human 5-HT1D receptor is determined to be 70% that of 5-HT in a cytosensor cell-based assay compared with 84% for that of Sumatriptan.
PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds.
| Animal Model: | Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode |
| Dosage: | 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg |
| Administration: | Intravenous injection |
| Result: | Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses. |