Effect of LY53857, a selective 5HT2 receptor antagonist, on 5HT-induced increases in cutaneous vascular permeability in rats.
Both serotonin and histamine increased cutaneous vascular permeability in rats; however, serotonin was approximately 100-fold more potent than histamine. LY53857 (0.1 and 1.0 mg/kg, i.p.), a selective 5HT2 receptor antagonist, blocked serotonin- but not histamine-induced increases in cutaneous vascular permeability. the alpha 1 receptor antagonist, prazosin, did not significantly affect increases in vascular permeability produced by serotonin. These data extend previous studies with LY53857 by further documenting its selectivity as a 5HT2 receptor antagonist. In addition, these results with a selective 5HT2 receptor antagonist provide evidence that 5HT2 receptor activation may be the predominant mechanism associated with vascular permeability changes induced by serotonin.
Cohen
M L
ML
Department of Cardiovascular Pharmacology, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.
Schenck
K
K
D000818:Animals; D002199:Capillary Permeability / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004873:Ergolines / Q000494:pharmacology*; D006632:Histamine / Q000008:administration & dosage / Q000494:pharmacology; D008297:Male; D011224:Prazosin / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000187:drug effects / Q000502:physiology*; D012701:Serotonin / Q000008:administration & dosage / Q000494:pharmacology*; D012702:Serotonin Antagonists; D012867:Skin / Q000098:blood supply*
D004873:Ergolines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D012701:Serotonin; D006632:Histamine; C032663:LY 53857; D011224:Prazosin