Vasopressin V1a receptor (AVPR1A) (AVPR1A)

The Vasopressin V1a receptor (AVPR1A) is a G protein-coupled receptor that primarily mediates the pressor effects of arginine vasopressin (AVP) through the Gq/11 signaling pathway, leading to increased intracellular calcium and smooth muscle contraction [1, 2]. It is widely expressed in the vascular smooth muscle, liver, kidney, and various regions of the brain, where it plays a critical role in regulating blood pressure, platelet aggregation, and social behaviors [1, 3]. In cardiovascular pathology, overactivation of V1aR contributes to excessive vasoconstriction and heart failure progression, making it a target for antagonistic therapies [2, 4]. Conversely, V1aR agonists like terlipressin are utilized in clinical settings to manage vasodilatory shock by restoring vascular tone [5]. Beyond its peripheral roles, the receptor is implicated in neuropsychiatric conditions such as autism and social anxiety, leading to the development of selective antagonists like balovaptan for behavioral modulation [2, 3]. Therapeutic intervention must carefully balance systemic vascular effects with potential central nervous system impacts [4]. Sources: [1] UniProt (P37288); [2] IUPHAR/BPS Guide to Pharmacology; [3] NCBI Gene (552); [4] PubChem (AVPR1A); [5] Manning M, et al. (2012) Vasopressin and oxytocin agonists and antagonists.

Other names

Arginine vasopressin receptor 1AV1aRAVPR1Vascular arginine vasopressin receptorAntidiuretic hormone receptor 1A

Competitive antagonism of arginine vasopressin binding to inhibit Gq-mediated signaling or selective agonism to induce vasoconstriction [2, 5].