On the bioactive conformation of NAN-190 (1) and MP3022 (2), 5-HT1A receptor antagonists

…, J Borycz, S Charakchieva-Minol…

文献索引：Paluchowska, Maria H.; Mokrosz, Maria J.; Bojarski, Andrzej; Wesolowska, Anna; Borycz, Jolanta; Charakchieva-Minol, Sijka; Chojnacka-Wojcik, Ewa Journal of Medicinal Chemistry, 1999 , vol. 42, # 24 p. 4952 - 4960

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被引用次数: 40

摘要

Structural modifications of 1, a postsynaptic 5-HT1A receptor antagonist, provided its flexible (8, 12) and rigid (7, 9, 11, 13) analogues. Compounds 7, 8, 9, and 11 showed high 5-HT1A receptor affinity (K i= 4-72 nM). They acted as 5-HT1A postsynaptic receptor antagonists, since, like 1, they inhibited the behavioral syndrome, ie, flat body posture (FBP) and forepaw treading (FT), in reserpine-pretreated rats as well as the lower lip retraction (LLR) in rats, ...