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208109-38-0

中文名称 F 13714
英文名称 Methanone, (3-chloro-4-fluorophenyl)[4-fluoro-4-[[[[5-methyl-6-(methylamino)-2-pyridinyl]methyl]amino]methyl]-1-piperidinyl]-
CAS 208109-38-0
分子式 C21H25ClF2N4O
分子量 422.9
MOL 文件 208109-38-0.mol
208109-38-0 结构式 208109-38-0 结构式

基本信息

中文别名
F 13714
英文别名
Methanone, (3-chloro-4-fluorophenyl)[4-fluoro-4-[[[[5-methyl-6-(methylamino)-2-pyridinyl]methyl]amino]methyl]-1-piperidinyl]-

物理化学性质

沸点583.8±50.0 °C(Predicted)
密度1.29±0.1 g/cm3(Predicted)
储存条件2-8°C
溶解度DMSO: 2mg/mL, clear
酸度系数(pKa)7.97±0.20(Predicted)
形态powder
颜色white to beige

应用领域

用途一
F13714 is a Serotonin 5-HT1A Receptor Agonist. F13714 shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress. F13714 has a high affinity (0.1 nM) and selectivity for 5-HT(1A) receptors. In vitro (18)F-F13714 binding in rats was consistent with the known 5-HT(1A) receptors distribution (hippocampus and cortical areas) and was particularly high in the dorsal raphe. In vitro binding of (18)F-F13714 was blocked in a dose-dependent fashion by WAY100635, the prototypical 5-HT(1A) antagonist, and by the endogenous agonist, serotonin (5-HT). Addition of Gpp(NH)p also inhibited in vitro (18)F-F13714 binding, consistent with a preferential binding of the compound to G-protein-coupled receptors. Ex vivo tissue measurements in rat revealed an absence of brain radioactive metabolites.

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概述
F 13714 (F 14679) 是一种典型的 5-HT1A 激动剂,pKi 为 10.23。F 13714 诱导较大的 Ca2+ 反应。
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