title: Response of hamster cheek pouch microcirculation to endothelin and endothelin receptor antagonists.
abstract: Our goal was to examine the effects of endothelin-1 and endothelin-3 on hamster cheek pouch arterioles in vivo in the absence and presence of endothelin receptor antagonists. Endothelin-1 (0.1, 1.0 and 10 pM) and endothelin-3 (0.1 and 1.0 nM) produced dose-related constriction of cheek pouch arterioles which was inhibited by the endothelin ETAB receptor antagonist PD 142893 (Ac-D-Dip-Leu-Asp-Ile-Ile-Trp) and endothelin ETA receptor antagonist PD 147953 [FR 139317: (hexahydro-1H-azepinyl)carbonyl-Leu-(N-Me)-D-Trp- D-2-Pya]. The thromboxane analogue, U-46619 (0.1 and 1.0 nM) also produced dose-related constriction of cheek pouch arterioles, but in contrast to endothelin-1 and endothelin-3 this vasoconstriction was not abolished by endothelin receptor antagonists. These findings suggest that endothelin-1 and endothelin-3 produce marked constriction of cheek pouch arterioles which appears to be mediated by activation of endothelin ETA receptors.
authors.affiliation: Department of Physiology and Biophysics, University of Nebraska Medical Center, Omaha 68198-4575, USA.
authors.forename: W G
authors.initials: WG
authors.lastname: Mayhan
authors.forename: I
authors.initials: I
authors.lastname: Rubinstein
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001381:Azepines / Q000494:pharmacology; D002610:Cheek / Q000098:blood supply; D006224:Cricetinae; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000494:pharmacology*; D007211:Indoles / Q000494:pharmacology; D008297:Male; D008647:Mesocricetus; D008833:Microcirculation / Q000187:drug effects*; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000494:pharmacology
chemical_list: D001381:Azepines; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D007211:Indoles; D009842:Oligopeptides; C079574:FR 139317; C076213:PD 142893