Binding of [(3)H]prazosin to alpha(1A)- and alpha(1B)-adrenoceptors, and to a cimetidine-sensitive non-alpha(1) binding site in rat kidney membranes.
[(3)H]Prazosin bound to alpha(1A)- and alpha(1B)-adrenoceptors, as well as to a cimetidine-sensitive non-alpha(1)-adrenoceptor binding site in rat kidney membranes. An experimental design is presented where the alpha(1)-adrenoceptors are selectively exposed by blocking the non-alpha(1) binding site with 60 microM cimetidine. Conversely, the non-alpha(1) binding site can be selectively exposed by blocking the alpha(1)-adrenoceptors with 600 nM metitepine. The identity of the non-alpha(1) binding site for [(3)H]prazosin in the rat kidney, herein pharmacologically characterized by 33 competing substances, is still unknown.
Mugisha
Paul
P
Department of Physiology, Uppsala University, Box 572 BioMedical Centre, 751 23 Uppsala, Sweden.
Gründemann
Dirk
D
Schömig
Edgar
E
Uhlén
Staffan
S
D000317:Adrenergic alpha-Antagonists / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D001665:Binding Sites; D002462:Cell Membrane / Q000378:metabolism; D002478:Cells, Cultured; D002927:Cimetidine / Q000494:pharmacology*; D007668:Kidney / Q000378:metabolism* / Q000648:ultrastructure; D008297:Male; D011224:Prazosin / Q000378:metabolism / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D018340:Receptors, Adrenergic, alpha-1 / Q000378:metabolism*; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism
D000317:Adrenergic alpha-Antagonists; D018340:Receptors, Adrenergic, alpha-1; D018341:Receptors, Adrenergic, alpha-2; D002927:Cimetidine; D011224:Prazosin