Synthesis, affinity at 5-HT2A, 5-HT2B and 5-HT2C serotonin receptors and structure-activity relationships of a series of cyproheptadine analogues.

MA HONRUBIA, J Rodriguez, R Dominguez…

Index: Honrubia, Maria Angeles; Jesus, Rodriguez; Dominguez, Rosa; Lozoya, Estrella; Manaut, Francesc; Seijas, Julio A.; Villaverde, Maria Carmen; Calleja, Jose M.; Cadavid, Maria Isabel; Maayani, Saul; Sanz, Ferran; Loza, Maria Isabel Chemical and Pharmaceutical Bulletin, 1997 , vol. 45, # 5 p. 842 - 848

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Citation Number: 11

Abstract

Cyproheptadine is a drug that shows high affinity for type 2 (5-HT 2) receptors. We studied a series of compounds obtained by modification of the tricyclic system of Cyp ( dibenzocycloheptadiene): 2f (thioxanthene), 2g (xanthene), 2h ( dihydrodibenzocycloheptadiene), 2j (diphenyl), 2i (fluorene), and 3b (phenylmethyl). Their activities at the rat cerebral cortex 5-HT 2A receptor were (pK i±SEM): 8.80±0.11 (Cyp), ...