SML3509
F13714
≥95% (HPLC)
别名:
(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
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About This Item
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生化/生理作用
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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
W Koek et al.
European journal of pharmacology, 420(2-3), 103-112 (2001-06-16)
To examine further the hypothesis that the magnitude of the intrinsic activity of agonists at 5-HT1A receptors determines the magnitude of their psychotropic activity, we studied the relationship between the maximal receptor activation produced by various 5-HT1A receptor ligands and
Adrian Newman-Tancredi et al.
Neurochemical research, 43(5), 1035-1046 (2018-03-25)
Peak-dose dyskinesia is associated with the dramatic increase in striatal dopamine levels that follows L-DOPA administration. The 'false neurotransmitter' hypothesis postulates that the latter is likely due to an aberrant processing of L-DOPA by serotonergic neurons. In keeping with this
H Iderberg et al.
Neuropharmacology, 93, 52-67 (2015-02-04)
Serotonin 5-HT1A receptor agonists reduce L-DOPA-induced dyskinesia (LID) in animal models of Parkinson's disease (PD). Here, we compared the effects of novel 5-HT1A receptor 'biased agonists' on LID in hemiparkinsonian rats. F13714 preferentially activates pre-synaptic 5-HT1A autoreceptors. F15599 preferentially activates
N P van Goethem et al.
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.
M-B Assié et al.
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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