title: Effect of a 5-HT1 receptor agonist, CP-122,288, on oedema formation induced by stimulation of the rat saphenous nerve.
abstract: Neurogenic oedema formation in the rat hind paw skin induced by electrical stimulation of the saphenous nerve and measured by extravasation of [125I]-albumin, was inhibited by the 5-HT1B receptor agonist, CP-93,129, and the novel tryptamine analogue, CP-122,288. Significant inhibition of up to 66% of control was observed with CP-122,288 (2 x 10(-14) - 2 x 10(-7) mol kg-1) and CP-93,129 (5 x 10(-7) - 5 x 10(-6) mol kg-1), with the minimum effective dose for CP-122,288 being about 10(7) fold less than that for CP-93,129. Oedema formation induced by the intradermal administration of exogenous mediators (substance P and histamine) in rat dorsal skin was not inhibited by CP-122,288 (2 x 10(-10) mol kg-1). These results suggest that CP-122,288 is a potent inhibitor of neurogenic inflammation in rat skin and that the effect may be due to a prejunctional inhibition of neuropeptide release.
authors.affiliation: Pharmacology Group, King's College, London.
authors.forename: R
authors.initials: R
authors.lastname: Kajekar
authors.forename: P
authors.initials: P
authors.lastname: Gupta
authors.forename: N B
authors.initials: NB
authors.lastname: Shepperson
authors.forename: S D
authors.initials: SD
authors.lastname: Brain
mesh_terms: D000704:Analysis of Variance; D000818:Animals; D004487:Edema / Q000517:prevention & control*; D004558:Electric Stimulation; D008297:Male; D009443:Neuritis / Q000517:prevention & control; D009475:Neurons, Afferent / Q000187:drug effects; D011725:Pyridines / Q000494:pharmacology; D011758:Pyrroles / Q000494:pharmacology; D011759:Pyrrolidines / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D017366:Serotonin Receptor Agonists / Q000494:pharmacology*; D018170:Sumatriptan / Q000031:analogs & derivatives* / Q000494:pharmacology
chemical_list: D011725:Pyridines; D011758:Pyrroles; D011759:Pyrrolidines; D017366:Serotonin Receptor Agonists; C065046:3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo(3,2-b)pyrid-5-one; C085263:CP 122288; D018170:Sumatriptan