(S)-5-fluoro-8-hydroxy-2-(dipropylamino) tetralin: a putative 5-HT1A-receptor antagonist

SE Hillver, L Bjoerk, YL Li, B Svensson…

Index: Hillver, Sven-Erik; Bjoerk, Lena; Li, Yi-Lin; Svensson, Bjoern; Ross, Svante; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 6 p. 1541 - 1544

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Citation Number: 90

Abstract

I $!? R= F to abolish efficacy but not the affinity for 5-HTlA receptors. 12 Thus,(S)-5-fluoro-8- hydroxy-2-(dipropylamino)-tetralin [(S)-2] behaves as a 5-HTlA-receptor antagonist. This conclusion is corroborated by the ability of (8-2 to inhibit (R)-1-induced biochemical and behavioral changes in the rat in a dose-dependent manner. In contrast, racemic 2 is inactive in functional assays and (R)-2, although being of slightly lower potency than (R)-and (9-1, ...