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Pelanserin inhibition of serotonin‐induced phosphatidylinositol turnover and contraction in rabbit aorta
Author(s) -
VillalobosMolina Rafael,
Castillo Carlos,
Hong Enrique
Publication year - 1991
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430230311
Subject(s) - quipazine , methysergide , phosphatidylinositol , prazosin , ketanserin , contraction (grammar) , chemistry , serotonin , endocrinology , agonist , medicine , stimulation , pharmacology , antagonist , 5 ht receptor , receptor , biology , biochemistry , signal transduction
Stimulation of rabbit aortic rings with serotonin or quipazine increased the incorporation of [ 32 P]Pi into phosphatidylinositol (Pl) and induced a dose‐related contraction. The effects of serotonin and quipazine were blocked by 5‐HT 2 antagonists with the following order of potency: pelanserin = ketanserin ≫ methysergide. Indorenate, a 5‐HT 1 agonist, failed to modify phosphatidylinositol labeling in rabbit aorta but elicited a very weak contraction at high concentrations. Pelanserin blocked epinephrine‐stimulated phosphatidylinositol labeling, being two orders of magnitude less potent than prazosin. The results demonstrate that pelanserin is a potent antagonist of the stimulation of Pl labeling and vasoconstrictor effects of 5‐hydroxytryptamine and suggest that 5‐HT 2 blockade is involved as its major pharmacologic action.