Gosset Beta-adrenoceptor Overview
Beta-adrenoceptors (β-ARs) are a class of G protein-coupled receptors that mediate the effects of catecholamines, such as norepinephrine and epinephrine, throughout the body. There are three main subtypes: β1, β2, and β3. β1-ARs are primarily located in the heart and kidney and regulate heart rate, contractility, and renin release. β2-ARs are widely distributed in smooth muscle and mediate bronchodilation and vasodilation. β3-ARs are primarily found in adipose tissue and regulate lipolysis. These receptors are important therapeutic targets, with beta-blockers used to treat cardiovascular diseases and beta-agonists used as bronchodilators.
Mechanism of Action
Agonists stimulate adenylyl cyclase, increasing cAMP production. Antagonists block the receptor, preventing catecholamine binding and downstream signaling.
Biological Functions
Disease Associations
Safety Considerations
- Non-selective beta-blockers can cause bronchoconstriction in susceptible individuals
- Cardioselective beta-blockers can still affect β2 receptors at higher doses
- Beta-agonists can cause tremors and tachycardia
- Potential for drug interactions