title: CP-93,129, a potent and selective 5-HT1B receptor agonist blocks neurogenic plasma extravasation within rat but not guinea-pig dura mater.
abstract: Pretreatment with CP-93,129 blocked plasma extravasation in rat dura mater induced by electrical trigeminal ganglion stimulation when administered at greater than or equal to 140 nmol kg-1, i.v. but did not affect plasma leakage in guinea-pig at 460 or 1400 nmol kg-1. Sumatriptan, a 5-HT1D-like receptor agonist, blocked plasma extravasation in the guinea-pig model when administered at 7 nmol kg-1. In as much as CP-93,129 binds with micromolar affinities to 5-HT1A, 5-HT1C, 5-HT1D, and 5-HT2 recognition sites, and with nanomolar affinity to the 5-HT1B receptor subtype, blockade of plasma extravasation in the rat dura mater may be mediated by 5-HT1B receptors whereas the 5-HT1D receptor may be more relevant to the guinea-pig.
authors.affiliation: Stroke Research Laboratory, Massachusetts General Hospital, Harvard Medical School, Boston 02114.
authors.forename: T
authors.initials: T
authors.lastname: Matsubara
authors.forename: M A
authors.initials: MA
authors.lastname: Moskowitz
authors.forename: B
authors.initials: B
authors.lastname: Byun
mesh_terms: D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D002211:Capsaicin / Q000494:pharmacology; D004388:Dura Mater / Q000502:physiology*; D004558:Electric Stimulation; D006168:Guinea Pigs; D007211:Indoles / Q000494:pharmacology; D008024:Ligands; D008297:Male; D010949:Plasma / Q000502:physiology*; D011506:Proteins / Q000378:metabolism; D011725:Pyridines / Q000494:pharmacology*; D011758:Pyrroles / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000187:drug effects*; D012711:Serum Albumin, Radio-Iodinated; D013449:Sulfonamides / Q000494:pharmacology; D018170:Sumatriptan; D012668:Trigeminal Ganglion / Q000502:physiology; D014662:Vasoconstrictor Agents / Q000494:pharmacology
chemical_list: D007211:Indoles; D008024:Ligands; D011506:Proteins; D011725:Pyridines; D011758:Pyrroles; D011985:Receptors, Serotonin; D012711:Serum Albumin, Radio-Iodinated; D013449:Sulfonamides; D014662:Vasoconstrictor Agents; C065046:3-(1,2,5,6-tetrahydropyrid-4-yl)pyrrolo(3,2-b)pyrid-5-one; D018170:Sumatriptan; D002211:Capsaicin