Adrenoceptor alpha 2A (alpha-2A adrenergic receptor) (ADRA2A)

Adrenoceptor alpha 2A is a G protein-coupled receptor that mediates the inhibitory effects of the catecholamines norepinephrine and epinephrine in both the central and peripheral nervous system. It plays a key role in the negative feedback regulation of neurotransmitter release from sympathetic and central adrenergic neurons, and is implicated in cardiovascular regulation, sedation, analgesia, cognition, and multiple other physiological processes. The receptor is therapeutically targeted by a variety of drugs for conditions such as hypertension, ADHD, withdrawal syndromes, and as adjuncts in anesthesia. The ADRA2A gene encodes the alpha-2A subtype in humans. As with all GPCRs, the receptor acts by transducing extracellular signals into intracellular responses, often by inhibiting adenylyl cyclase and modulating ion channels.

Other names

Alpha-2A adrenergic receptorAlpha2A adrenoceptorAlpha2AARADRA2AAlpha-2AAR subtype C10Alpha2A/D-ARAlpha2-C10ADRAR

Agonists: activate presynaptic alpha-2A receptors, inhibit norepinephrine release, reduce sympathetic outflow, lower blood pressure, and cause sedation/analgesia. Antagonists: block inhibitory feedback, increase norepinephrine release, potentially increase alertness, and may disrupt sedation or hypotension. Modulation of adenylyl cyclase activity, potassium efflux, and ERK1/2 signaling.