179756-58-2

179756-58-2 structure

Name: Eptapirone
Chemical Name: 4-Methyl-2-{4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl}-1,2,4-triazinane-3,5-dione
CAS Number: 179756-58-2
Molecular Formula: C₁₆H₂₃N₇O₂
Molecular Weight: 345.40
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-03-08 01:56:19
Modify Date: 2024-01-17 01:03:59
F 11440 is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.Target: 5-HT1AThe affinity of F 11440 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, F 11440 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). F 11440, 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]

Name	4-Methyl-2-{4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl}-1,2,4-triazinane-3,5-dione
Synonyms	4-Methyl-2-{4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl}-1,2,4-triazinane-3,5-dione 1,2,4-Triazine-3,5(2H,4H)-dione, dihydro-4-methyl-2-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]- Eptapirone F 11440

Description	F 11440 is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.Target: 5-HT1AThe affinity of F 11440 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, F 11440 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). F 11440, 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]
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Neurological Disease
References	[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.