Vasopressin receptor (AVPR) (AVPR)

Vasopressin receptors (AVPRs) are a class of G protein-coupled receptors that mediate the physiological actions of arginine vasopressin (AVP), also known as antidiuretic hormone. There are three primary subtypes: V1a (AVPR1A), V1b (AVPR1B), and V2 (AVPR2). The V1a receptor is found in vascular smooth muscle and mediates vasoconstriction, while the V1b receptor is located in the anterior pituitary and regulates the release of adrenocorticotropic hormone (ACTH). The V2 receptor is predominantly expressed in the renal collecting ducts, where it plays a critical role in water reabsorption by triggering the insertion of aquaporin-2 water channels into the apical membrane. Dysregulation of these receptors is linked to several clinical conditions, including diabetes insipidus, syndrome of inappropriate antidiuretic hormone secretion (SIADH), and hyponatremia in heart failure or cirrhosis. Pharmacological agents targeting these receptors include V2 agonists like desmopressin for nocturnal enuresis and central diabetes insipidus, as well as V2 antagonists like tolvaptan for treating hyponatremia and slowing the progression of autosomal dominant polycystic kidney disease.

Other names

Arginine vasopressin receptorAntidiuretic hormone receptorADH receptorAVP receptorAVPR1AAVPR1BAVPR2

Drugs targeting vasopressin receptors act as either agonists or antagonists. V2 receptor agonists (e.g., desmopressin) mimic AVP to increase water reabsorption in the kidney. V2 receptor antagonists (vaptans) block AVP-mediated water reabsorption, promoting aquaresis (solute-free water excretion). V1a receptor agonists (e.g., terlipressin) induce vasoconstriction to increase blood pressure and reduce portal pressure.