Affinity of different alpha 1-agonists and antagonists for the alpha 1-adrenoceptors of rabbit and rat liver membranes.
In membranes prepared from rabbit liver, competition with [3H]prazosin by different alpha 1-agonists and antagonists revealed different affinities in comparison to the results obtained on rat liver membranes, and showed a good correlation with the affinity of the same compounds for the cloned alpha 1c-adrenoceptor subtype. The potencies observed on rat liver membranes were well correlated with the affinity observed for the cloned alpha 1b-adrenoceptors. These results confirm that rabbit and rat liver membranes preparations can be utilized to evaluate the affinity of compounds for these alpha 1-adrenergic subtypes.
Taddei
C
C
Research Department, Recordati S.p.A. Milano, Italy.
Poggesi
E
E
Leonardi
A
A
Testa
R
R
D000316:Adrenergic alpha-Agonists / Q000378:metabolism* / Q000494:pharmacology; D000317:Adrenergic alpha-Antagonists / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D002462:Cell Membrane / Q000187:drug effects / Q000648:ultrastructure; D007700:Kinetics; D008099:Liver / Q000187:drug effects / Q000378:metabolism / Q000648:ultrastructure*; D008297:Male; D011224:Prazosin / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley; D011942:Receptors, Adrenergic, alpha / Q000145:classification / Q000378:metabolism*; D014316:Tritium
D000316:Adrenergic alpha-Agonists; D000317:Adrenergic alpha-Antagonists; D011942:Receptors, Adrenergic, alpha; D014316:Tritium; D011224:Prazosin