Hj. Mersmann et al., BINDING OF AGONISTS AND ANTAGONISTS TO THE PORCINE ADIPOSE-TISSUE BETA-ADRENERGIC RECEPTOR(S), Comparative biochemistry and physiology. C. Comparative pharmacologyand toxicology, 106(3), 1993, pp. 725-732
1. Affinities of agonists for porcine adipose tissue beta-adrenergic r
eceptors, determined by competitive ligand binding with H-3-dihydroalp
renolol to crude adipose tissue membranes in vitro, varied from 50 tim
es > to 25 times < than isoproterenol. Affinities for antagonists vari
ed from 8 times > to 1000 times < propranolol. 2. Receptor affinity wa
s not related to the ability to stimulate or inhibit lipolysis, or to
the agonist or antagonist purported receptor subtype specificity. 3. M
odeling of ligand-binding data indicated more than one binding site fo
r several ligands. The assignment of beta-adrenergic subtypes to the i
ndividual binding sites was unclear because this would depend on the i
ndividual ligands used to establish binding sites.