beta-adrenoceptors as molecular targets in the treatment of hypertension.

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Ferguson SS, Feldman RD

beta-adrenoceptors as molecular targets in the treatment of hypertension.

Can J Cardiol. 2014 May;30(5 Suppl):S3-8. doi: 10.1016/j.cjca.2014.01.017. Epub 2014 Feb 12.

PubMed ID
24685403 [ View in PubMed
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Abstract

Regulation of sympathoadrenal activity has been a long-time target in the management of hypertension. Regulation of beta-adrenoceptor (betaAR) function has been the most therapeutically important of these targets. The development of effective antihypertensive treatments based on betaAR antagonism paralleled the elucidation of the molecular basis of beta-adrenergic effects by the family of betaARs, which are members of the G-protein-coupled receptor (GPCR) superfamily. betaARs serve as the extracellular face of the transmembrane signalling pathway that results in the consequent activation of heterotrimeric G-proteins and the activation of several other newly appreciated signalling molecules that include beta-arrestins and GPCR kinases (GRKs). The aggregate effect of the activation of these signalling pathways mediates the response to betaAR activation. Paradoxically, the hypertensive state is characterized by impaired betaAR responsiveness. This defect is common to many other receptor systems linked to the stimulator G protein (Gs) and adenylyl cyclase activation. This impairment is principally mediated by receptor-G-protein uncoupling, which has been linked to increased expression and activity of GRK2.

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