Abstract
The β 3-selective adrenergic receptor ligand BRL 37344 (BRL) was used to differentiate the presence and functional role of β-adrenergic receptor (βAR) subtypes in pig tissues. BRL did not stimulate adenylyl cyclase in membrane preparations or increase lipolysis from pig adipocytes. In contrast to some species, BRL appears to be a poor agonist for the pig βAR and is not a useful β 3AR ligand. Based on displacement of [ 3H]dihydroalprenolol binding, BRL exhibited a 100-fold selectivity for pig βAR subtypes in adipose and skeletal muscle membranes. The high affinity site was proposed to be the β 2AR. When used as an antagonist, BRL blockade of the high affinity site did not interfere with isoproterenol-stimulated lipolysis but did inhibit adenylyl cyclase activation. Results indicate that the high affinity βAR (β 2AR) is not linked to lipolysis, possibly due to intracellular compartmentalization. Therefore, βAR subtypes may have function-specific effects.
Published Version
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