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.
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callMore From: Comparative Biochemistry and Physiology. Part C: Comparative Pharmacology and Toxicology
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
