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… - Chemical and …, 1997 - jstage.jst.go.jp
抄録 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),
8.60±0.07 (2f), 8.40±0.02 (2g), 8.05±0.03 (2h), 7.87±0.12 (2j), 6.70±0.02 (2i) and 6.45±0.02 …
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),
8.60±0.07 (2f), 8.40±0.02 (2g), 8.05±0.03 (2h), 7.87±0.12 (2j), 6.70±0.02 (2i) and 6.45±0.02 …
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