中文名 | EPTAPIRONE |
英文名 | EPTAPIRONE |
别名 | F 11440游离态 化合物EPTAPIRONE 4-甲基-2-(4-(4-(嘧啶-2-基)哌嗪-1-基)丁基)-1,2,4-三嗪-3,5(2H,4H)-二酮 4-甲基-2- [4- [4-(2-嘧啶基)-1-哌嗪基]丁基] -1,2,4-三嗪-3,5(2H,4H) - 二酮 |
英文别名 | F11440 F 11440 F-11440 EPTAPIRONE Eptapirone(F11440) 4-Methyl-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,2,4-triazine-3,5(2H,4H)-dione 4-methyl-2-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)-1,2,4-triazine-3,5(2H,4H)-dione 1,2,4-Triazine-3,5(2H,4H)-dione, 4-methyl-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]- |
CAS | 179756-58-2 |
化学式 | C16H23N7O2 |
分子量 | 345.4 |
密度 | 1.35±0.1 g/cm3(Predicted) |
沸点 | 517.4±60.0 °C(Predicted) |
酸度系数 | 7.72±0.10(Predicted) |
存储条件 | Inert atmosphere,Room Temperature |
体外研究 | The affinity of Eptapirone (F11440) for 5-HT1Abinding sites (pKi, 8.33) was higher than that of buspirone (pKi , 7.50), and somewhat lower than that of flesinoxan (pKi , 8.91).In vivo, Eptapirone (F11440) was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone, in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats (measured by, for example, its ability to decrease hippocampal extracellular serotonin (5-HT) levels and to increase plasma corticosterone levels, respectively). Eptapirone (F11440), shown here to be a potent, selective, high efficacy 5-HT1Areceptor agonist, appears to have the potential to exert marked anxiolytic and antidepressant activity in humans.[1] |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.895 ml | 14.476 ml | 28.952 ml |
5 mM | 0.579 ml | 2.895 ml | 5.79 ml |
10 mM | 0.29 ml | 1.448 ml | 2.895 ml |
5 mM | 0.058 ml | 0.29 ml | 0.579 ml |
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