Vasopressin V1a receptor (V1aR) (V1aR)

The Vasopressin V1a receptor (V1aR), encoded by the Avpr1a gene in rats, is a G protein-coupled receptor (GPCR) primarily located in vascular smooth muscle, the liver, and the central nervous system [1, 2, 5]. It mediates the effects of arginine vasopressin (AVP) through the Gq/11 signaling pathway, leading to phospholipase C activation and increased intracellular calcium [2, 8, 16]. In the periphery, V1aR activation causes potent vasoconstriction, platelet aggregation, and hepatic glycogenolysis, while in the brain, it regulates complex social behaviors, including aggression, anxiety, and pair bonding [2, 8, 15, 17]. Due to its role in regulating vascular tone and cardiac remodeling, the V1a receptor is a significant therapeutic target for cardiovascular diseases such as hypertension and heart failure [7, 10, 16]. Additionally, its involvement in social cognition has made it a target for treating neuropsychiatric conditions like autism spectrum disorder and post-traumatic stress disorder [13, 14, 15]. Pharmacological agents targeting V1aR include selective antagonists like relcovaptan and balovaptan, as well as dual V1a/V2 antagonists like conivaptan [2, 4, 11, 13].

Other names

Arginine vasopressin receptor 1A [1, 2]Antidiuretic hormone receptor 1A [1, 2]Vascular/hepatic-type arginine vasopressin receptor [1, 2]AVPR1A [2, 8]AVPR V1a [1, 2]

The V1a receptor primarily signals through the Gq/11 protein-coupled pathway, activating phospholipase C (PLC) to generate inositol trisphosphate (IP3) and diacylglycerol (DAG), which increases intracellular calcium levels [2, 8, 16]. Drugs targeting this receptor act as either antagonists to block vasoconstriction and modulate social behavior, or as agonists to induce pressor effects and enhance myocardial contractility [7, 10, 11, 15].