title: [3H]CGP-12177 binding to beta-adrenoceptors of intact bovine mononuclear leukocytes.
abstract: Saturation and inhibition binding studies, using [3H]CGP-12177 as radioligand, reveal the presence of a single class of beta-adrenoceptors on intact bovine mononuclear leukocytes. Receptor binding is inhibited by beta-adrenergic agonists with a rank order of potency (-)-isoproterenol > (-)-epinephrine > (-)-norepinephrine, indicating that the receptors are of the beta 2-subtype. By Scatchard analysis, the mean receptor density was 707 +/- 168 receptors/cell and the dissociation constant was 0.89 +/- 0.47 nM. Specific binding was very high and amounted to 80-90%. It is concluded that [3H]CGP-12177 is a promising compound for the reliable determination of the binding characteristics of bovine mononuclear leukocytes.
authors.affiliation: Department of Veterinary Physiology, Faculty of Veterinary Medicine, University of Ghent, Belgium.
authors.forename: M
authors.initials: M
authors.lastname: Vermeir
authors.forename: E
authors.initials: E
authors.lastname: Roets
authors.forename: C
authors.initials: C
authors.lastname: Burvenich
mesh_terms: D000262:Adenylyl Cyclases / Q000378:metabolism; D000319:Adrenergic beta-Antagonists / Q000378:metabolism*; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002417:Cattle; D002462:Cell Membrane / Q000187:drug effects / Q000201:enzymology; D005260:Female; D066298:In Vitro Techniques; D007700:Kinetics; D009504:Neutrophils / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism*; D011412:Propanolamines / Q000378:metabolism*; D011943:Receptors, Adrenergic, beta / Q000378:metabolism*
chemical_list: D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; D000262:Adenylyl Cyclases; C033394:CGP 12177