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CAS No.: 179756-58-2

Eptapirone Catalog No. CSN17354

Synonyms: F 11440;AJ-97166;L-0068

F 11440 is a potent, selective and high efficacy 5-HT1A receptor agonist with pKi value of 8.33.

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生物活性

描述Major Depressive Disorder (MDD) is a highly prevalent psychiatric diagnosis that is associated with a high degree of morbidity and mortality. Serotonergic dysfunction, specifically of the serotonin (5-HT) 1A receptor, plays a key role in the development of MDD^[2]. F11440, owing marked anxiolytic and antidepressant potential, is a potent, selective and highly effective 5-HT1A receptor agonist with a pK_i of 8.33. In HeLa cells expressing human 5-HT1A receptors, F 11440 decreased the forskolin-induced increase in AMP, and was found to have an intrinsic activity of 1.0 relative to that of 5-HT based on its maximal effect. In vivo, F 11440 was 30- to 60-fold more potent than buspirone, and 4- to 20-fold more potent than flesinoxan in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats. Moreover, F 11440 produced anxiolytic- and antidepressant-like effects in animal models (i.e., increased punished responding in a pigeon conflict procedure and decreased immobility in a rat forced swimming test, respectively)^[3]. Coadministration of F 11440 (2.5 mg/kg p.o.) and Sibutramine (10 mg/kg p.o.; a noradrenaline and serotonin reuptake inhibitor) attenuated sibutramine-induced hypertension and tachycardia without altering its food intake effects indicating that 5-HT1A activation by F 11440 can counter the undesirable cardiovascular effects resulting from increased sympathetic activity^[4].
参考文献

[1] Koek W, Patoiseau JF, 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.
[2] The 5-HT1A Receptor in Major Depressive Disorder
[3] F 11440, a Potent, Selective, High Efficacy 5-HT1A Receptor Agonist With Marked Anxiolytic and Antidepressant Potential
[4] 5-HT(1A) Activation Counteracts Cardiovascular but Not Hypophagic Effects of Sibutramine in Rats

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8952 mL
- 14.4760 mL
- 28.9520 mL
- 5 mM
- 0.5790 mL
- 2.8952 mL
- 5.7904 mL
- 10 mM
- 0.2895 mL
- 1.4476 mL
- 2.8952 mL

技术信息

CAS号

179756-58-2

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H23N7O2

运输

蓝冰

分子量

345.40

别名

F 11440;AJ-97166;L-0068

溶解度

DMSO	107.0 mg/mL (309.8 mM)
Water	insoluble

动物实验配方

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