(3-Chloro-4-fluorophenyl)-(4-fluoro-4-{[(5-methyl-6-methylaminopyridin-2-ylmethyl)amino]methyl}piperidin-1-yl)methanone, 1-(3-Chloro-4-fluorobenzoyl)-4-fluoro-N-[[5-methyl-6-(methylamino)-2-pyridinyl]methyl]-4-piperidinemethanamine, F 13714, F13714
F13714 is an orally active, high-affinity, potent, biased serotonin receptor 5-HT1A agonist (pKi = 10.12 against 0.2 nM (±)-8-OH-DPAT binding to rat cortex tissue). F13714 inhibits 100 μM forskolin-induced cAMP accumulation in human 5-HT1A-expressing HeLa cells (pIC50 = 8.67) and displays antidepressant efficacy in vivo (ED50 = 0.05 mg/kg p.o., Emax >80%; rat forced swimming). F13714 and F15599 display differential biased agonism and, when administerd in vivo, F13714 preferentially activates raphe-located autoreceptors, while F15599 preferentially activates post-synaptic heteroreceptors.
Orally active, high-affinity, potent, biased serotonin receptor 5-HT1A agonist with a differential mode of action as F15599 in vitro and in vivo.
The serotonin (5-HT) deficiency hypothesis of aggression is being seriously challenged by pharmacological data showing robust anti-aggressive effects of 5-HT1A receptor agonists in dose ranges that concomitantly inhibit 5-HT neurotransmission. Hence, an adequate interpretation of the role of 5-HT activity
British journal of pharmacology, 172(10), 2532-2543 (2015-01-13)
Pattern separation, that is, the formation of distinct representations from similar inputs, is an important hippocampal process implicated in cognitive domains like episodic memory. A deficit in pattern separation could lead to memory impairments in several psychiatric and neurological disorders.
The subject of the present study was the functional and pharmacological characterization of human 5-HT(1A) receptor regulation of ion channels in Xenopus oocytes. Activation of the heterologously expressed human 5-HT(1A) receptor induced two distinct currents in Xenopus oocytes, consisting of
Journal of medicinal chemistry, 42(9), 1648-1660 (1999-05-07)
The aim of this work was to improve the oral bioavailability of a recently discovered, novel structural class of 5-HT1A receptor agonists: aryl-{[4-(6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1 -yl-metha none. Incorporation of a fluorine atom in the beta-position to the amino function in the side
British journal of pharmacology, 149(2), 170-178 (2006-08-22)
Desensitization of somatodendritic 5-HT(1A) receptors is involved in the mechanism of action of several antidepressants, but the rapidity of this effect and the amount of agonist stimulation needed are unclear. We evaluated the capacity of the high-efficacy 5-HT(1A) agonist, F13714
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