Localization of (-)-[125I]cyanopindolol binding in guinea-pig heart: characteristics of non-beta-adrenoceptor related binding in cardiac pacemaker and conducting regions.
Receptor autoradiography was used in guinea-pig heart to locate binding sites for the beta-adrenoceptor ligand (-)[125I]cyanopindolol (CYP) resistant to blockade by the beta-adrenoceptor antagonist (-)-propranolol (1 microM). Highly localized binding was observed to regions closely associated with the sinoatrial node, atrioventricular node and bundle of His but was not observed on myocardial, pacemaker, conducting cells or adipose tissue. Free [125I] also bound to identical sites. Binding was enhanced in the presence of ascorbic acid but was completely inhibited by (-)-isoprenaline (100 microM), serotonin (5-HT) (10 microM) and phentolamine (10 microM).
Molenaar
P
P
Department of Pharmacology, University of Melbourne, Parkville, Vic., Australia.
Kompa
A R
AR
Roberts
S J
SJ
Pak
H S
HS
Summers
R J
RJ
D000526:Alprenolol / Q000494:pharmacology; D000818:Animals; D001205:Ascorbic Acid / Q000494:pharmacology; D001665:Binding Sites; D004983:Ethanolamines / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D006220:Haloperidol / Q000494:pharmacology; D006329:Heart Conduction System / Q000378:metabolism*; D007545:Isoproterenol / Q000494:pharmacology; D008297:Male; D009206:Myocardium / Q000378:metabolism*; D009195:Peroxidase / Q000378:metabolism; D010646:Phentolamine / Q000494:pharmacology; D010869:Pindolol / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D011412:Propanolamines / Q000494:pharmacology; D011433:Propranolol / Q000494:pharmacology; D011485:Protein Binding; D011943:Receptors, Adrenergic, beta / Q000187:drug effects; D012701:Serotonin / Q000494:pharmacology; D013876:Thiophenes; D014132:Trachea / Q000187:drug effects / Q000378:metabolism
D004983:Ethanolamines; D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; D013876:Thiophenes; D012701:Serotonin; C047975:cyanopindolol; C057368:BRL 37344; D000526:Alprenolol; D011433:Propranolol; C005632:tertatolol; D010869:Pindolol; D009195:Peroxidase; D006220:Haloperidol; D007545:Isoproterenol; D001205:Ascorbic Acid; D010646:Phentolamine; C047411:cimaterol