F-11440

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 5-HT1A 受体激动剂，Ki 为 4.8 nM，pKi 为 8.33。

A potent, selective 5-HT1A receptor agonist with Ki of 4.8 nM, pKi of 8.33; shows ≥shows 100-fold higher affinity for the other serotonin receptor subtypes, and has no detectable antidopaminergic activity and antihistaminergic activity; decreases the forskolin-induced increase in AMP in HeLa cells expressing human 5-HT1A receptors; produces anxiolytic- and antidepressant-like effects in animal models.Anxiety Phase 1 Discontinued(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.

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.

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Eptapirone

GPCR/G Protein

5-HT Receptor

5-HT1A

Neurological Disease

Anxiety

179756-58-2

345.3995

C16H23N7O2

>98% (HPLC)

DMSO: 6 mg/mL (Need ultrasonic)

O=C(N1C)N(CCCCN2CCN(C3=NC=CC=N3)CC2)N=CC1=O

1,2,4-Triazine-3,5(2H,4H)-dione, 4-methyl-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-

(-20℃)

With Ice Pack

≥ 2 years