Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors

B Vacher, B Bonnaud, P Funes, N Jubault…

文献索引：Vacher, Bernard; Bonnaud, Bernard; Funes, Philippe; Jubault, Nathalie; Koek, Wouter; Assie, Marie-Bernadette; Cosi, Cristina; Kleven, Mark Journal of Medicinal Chemistry, 1999 , vol. 42, # 9 p. 1648 - 1660

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被引用次数: 88

摘要

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-methanone. Incorporation of a fluorine atom in the β-position to the amino function in the side chain led to analogues that exhibited, in general, enhanced and long- lasting 5-HT1A agonist activity in rats after oral administration. Location of the fluorine ...