Eptapirone (Synonyms: F 11440)
目录号: PL04981 纯度: ≥98%
CAS No. :179756-58-2
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中文名称
Eptapirone
中文别名
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;EPTAPIRONE
英文名称
Eptapirone
英文别名
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;EPTAPIRONE;Eptapirone free base;F11440;F-11440;L-0068;F 11440;Eptapirone [INN];3M824XRO8N;Eptapirone (INN);4-Methyl-2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-as-triazine-3,5(2H,4H)-dione.;4-methyl-2-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-1,2,4-triazine-3,5-dione
Cas No.
179756-58-2
分子式
C16H23N7O2
分子量
345.40
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Eptapirone (F11440) 是一种强效,选择性,疗效高的 5HT1A 受体激动剂, 有显著的抗焦虑和抗抑郁潜力。
生物活性
Eptapirone (F11440) is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
性状
Solid
IC50 & Target[1][2]
5-HT1A Receptor
体外研究(In Vitro)
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] has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Koek W, et al. F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. J Pharmacol Exp Ther. 1998 Oct;287(1):266-83.
溶解度数据
In Vitro: DMSO : 250 mg/mL (723.80 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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