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179756-58-2

中文名稱 F 11440
英文名稱 EPTAPIRONE
CAS 179756-58-2
分子式 C16H23N7O2
分子量 345.4
MOL 文件 179756-58-2.mol
更新日期 2024/12/24 22:28:18
179756-58-2 結(jié)構(gòu)式 179756-58-2 結(jié)構(gòu)式

基本信息

中文別名
F 11440游離態(tài)
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
英文別名
F 11440
EPTAPIRONE
F-11440
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]-
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)517.4±60.0 °C(Predicted)
密度1.35±0.1 g/cm3(Predicted)
儲(chǔ)存條件Inert atmosphere,Room Temperature
溶解度DMF:10.0(Max Conc. mg/mL);28.95(Max Conc. mM)
酸度系數(shù)(pKa)7.72±0.10(Predicted)
形態(tài)結(jié)晶固體
顏色White to off-white

常見問題列表

生物活性
Eptapirone (F11440) 是一種強(qiáng)效,選擇性,療效高的 5HT1A 受體激動(dòng)劑, 有顯著的抗焦慮和抗抑郁潛力。
靶點(diǎn)

5-HT 1A Receptor

體外研究

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]

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