Regulation of the Human A₁ Adenosine Receptor Gene

Abstract

Adenosine is a physiologically important metabolite and a clinically useful drug. Endogenous release of adenosine mediates a variety of physiologic effects in a wide range of organ systems [1]. These effects are largely transduced via specific adenosine receptors (AR). At present, four subtypes of adenosine receptors have been reported in the literature—A₁, A_2a, A_2b, and A3 receptors—and all have been cloned. The A₁ receptor mediates a wide range of physiologic effects, including inhibition of neurotransmitter release, suppression of heart rate and contractility, inhibition of lipolysis, and regulation of smooth muscle tone [2]. Activation of the A₁ receptor may produce a dramatic cardioprotective effect against ischemic heart damage [3]. Factors that regulate A₁ receptor expression in tissues thus become critically important in understanding physiologic and therapeutic processes.