Antagonism by some ergot derivatives of 5-HT-induced vasoconstriction.
The ability of a number of ergot derivatives to inhibit 5-hydroxytryptamine (5-HT)-induced vasoconstriction was examined in the perfused rat mesenteric artery preparation. 5-HT produced an increase in perfusion pressure indicative of vasoconstriction. The ergot derivatives inhibited the 5-HT-induced vasoconstriction in a manner that was predominantly not competitive in nature. As 5-HT2 antagonists the ergot derivatives ranged in potency from CQ 32-084 which abolished the 5-HT2 receptor mediated response at a concentration of 10 nM to LY-141865 which was inactive up to a concentration of 10 microM.
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Conolan
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Taylor
D000818:Animals; D004873:Ergolines / Q000494:pharmacology; D004876:Ergot Alkaloids / Q000494:pharmacology*; D005260:Female; D066298:In Vitro Techniques; D008297:Male; D008638:Mesenteric Arteries / Q000187:drug effects / Q000502:physiology; D010477:Perfusion; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000187:drug effects / Q000502:physiology; D012701:Serotonin / Q000494:pharmacology*; D012702:Serotonin Antagonists / Q000494:pharmacology; D014661:Vasoconstriction / Q000187:drug effects*
D004873:Ergolines; D004876:Ergot Alkaloids; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C031648:etisulergine; D012701:Serotonin