Arginine vasopressin receptor 1A (AVPR1A) and Arginine vasopressin receptor 2 (AVPR2) (AVPR1A/AVPR2)

Vasopressin receptors V1a and V2 are G protein-coupled receptors (GPCRs) that mediate the physiological effects of the hormone arginine vasopressin (AVP) [6, 8]. The V1a receptor (AVPR1A) is primarily located in vascular smooth muscle, where it induces vasoconstriction via the Gq/11 signaling pathway, and in the brain, where it influences social behavior and anxiety [14, 18]. The V2 receptor (AVPR2) is predominantly found in the renal collecting ducts, where it signals through the Gs pathway to promote the insertion of aquaporin-2 water channels, facilitating water reabsorption and maintaining fluid balance [11, 12]. These receptors are key therapeutic targets for conditions involving fluid imbalance, such as hyponatremia and syndrome of inappropriate antidiuretic hormone secretion (SIADH) [1, 4]. Dual V1a/V2 antagonists like conivaptan are used to promote aquaresis and increase serum sodium levels in hospitalized patients [2, 5]. Selective V2 agonists like desmopressin are utilized in the management of central diabetes insipidus and certain bleeding disorders like Hemophilia A [11, 12]. Safety considerations for drugs targeting these receptors include the risk of osmotic demyelination syndrome if sodium levels are corrected too rapidly [1, 2]. Overall, these receptors play a vital role in cardiovascular and renal homeostasis and are central to the management of various water-electrolyte disorders [8, 13].

Other names

V1a receptorV2 receptorV1aRV2RAVPR1AAVPR2Antidiuretic hormone receptorVasopressin V1a and V2 receptors

V2 receptor antagonism inhibits the insertion of aquaporin-2 channels in the renal collecting ducts, promoting electrolyte-free water excretion (aquaresis); V1a receptor antagonism inhibits vasopressin-mediated vasoconstriction; V2 receptor agonism stimulates water reabsorption and the release of coagulation factors VIII and von Willebrand factor.