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Serotonin-induced relaxation in canine coronary artery smooth muscle

DJ Cushing and ML Cohen

Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana.

Serotonin (5-HT) is a potent contractile agonist in canine coronary artery devoid of endothelium; however, in higher concentrations 5-HT produces concentration-dependent relaxation by activating an as yet uncharacterized receptor. This study explored the possibility that 5-HT- induced relaxation was mediated by interaction with a member of the 5- HT1, 5-HT2, 5-HT3, or 5-HT4 receptor family. 5-HT, 5- carboxamidotryptamine and 5-methoxytryptamine produced concentration- dependent relaxation in vitro in tissues precontracted with prostaglandin F2 alpha (10 microM). The agonist rank order potency for relaxation was 5-carboxamidotryptamine > 5-HT > 5-MeOT. 8- hydroxydipropylaminotetralin (8-OH-DPAT), dipropyl-5-CT, 5- methyltryptamine, sumatriptan, alpha-methyl-5-HT and 2-methyl-5-HT did not produce significant relaxation. The 5-HT1/beta adrenergic receptor antagonist propranolol (1 microM) did not antagonize 5-HT-induced relaxation. 5-HT-induced relaxation was not blocked by tetrodotoxin (0.3 microM), suggesting that neuronal depolarization to release mediators from nerves was not responsible for the relaxation. Neither ketanserin (1 microM) nor ritanserin (1 microM) antagonized 5-HT- induced relaxation, suggesting that 5-HT2 and 5-HT1C receptors do not mediate relaxation. ICS 205-930 (10 microM), a 5-HT3/5-HT4 receptor antagonist, shifted the 5-HT concentration-response curve modestly to the right (pKB = 5.1 +/- 0.1). Cisapride, a 5-HT4 receptor agonist, was not effective either as an agonist (up to 10 microM), or as an antagonist (1 microM) of 5-HT-induced relaxation.(ABSTRACT TRUNCATED AT 250 WORDS)

Volume 263, Issue 1, pp. 123-129, 10/01/1992
Copyright © 1992 by American Society for Pharmacology and Experimental Therapeutics




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