Arginine vasopressin receptor 1A (AVPR1A) and Arginine vasopressin receptor 1B (AVPR1B) (AVPR1A/AVPR1B)

The Vasopressin V1a and V1b receptors are G protein-coupled receptors (GPCRs) that mediate the physiological effects of arginine vasopressin (AVP) through the Gq/11 signaling pathway. The V1a receptor (AVPR1A) is predominantly found in vascular smooth muscle, where it induces vasoconstriction, and in the brain, where it modulates complex social behaviors and emotional regulation (UniProt P37288). The V1b receptor (AVPR1B), often referred to as the V3 receptor, is primarily expressed in the anterior pituitary and plays a critical role in the stress response by stimulating the secretion of adrenocorticotropic hormone (ACTH) (PubMed: 11906001). These receptors are significant therapeutic targets for cardiovascular conditions like heart failure and hyponatremia, as well as neuropsychiatric disorders including anxiety, depression, and autism spectrum disorder (PubMed: 25833129). Drugs interacting with these receptors include conivaptan, a dual V1a/V2 antagonist used for hyponatremia, and selective antagonists like relcovaptan (V1a) and nelivaptan (V1b) (PubChem CID 443871). Clinical management of these targets requires careful monitoring of blood pressure and electrolyte balance due to their potent effects on vascular tone and the HPA axis (StatPearls: Vasopressin). Research continues into the role of V1a in social communication deficits, with agents like balovaptan being investigated for autism (PubMed: 30655495).

Other names

V1a receptorV1b receptorV3 receptorAntidiuretic hormone receptor 1AAntidiuretic hormone receptor 1BV1aRV1bR

Drugs targeting these receptors typically act as antagonists to block the binding of arginine vasopressin, thereby inhibiting the Gq-protein signaling pathway. This results in decreased vascular resistance (V1a) and reduced secretion of adrenocorticotropic hormone (V1b). Conversely, agonists like terlipressin activate these receptors to induce vasoconstriction for the treatment of conditions like hepatorenal syndrome.