Vasopressin (VP) receptors are receptors that mediate the functions of arginine vasopressin (AVP). The VP receptors are members of the G-protein coupled receptor (GPCR) superfamily, consisting of seven hydrophobic transmembrane α helices joined by an extracellular N-terminal domain and a cytoplasmatic C-terminal domain. Based on the second messenger to which they are coupled, VP receptors are classified into V1a, V1b, and V2 subtypes. The V1a and V1b receptors are linked to the phosphoinositol signaling pathway via Gaq/11 GTP-binding proteins that activate phospholipase C activity, with intracellular calcium acting as the second messenger. In contrast, V2 receptors are linked to the adenylate cyclase signaling pathway via Gs-binding proteins, with intracellular cAMP acting as the second messenger.
Moreover, these subtypes differ in localization and function. V1a receptors are widely distributed and V1b receptors are mainly expressed in the anterior pituitary and the brain. V2 receptors are expressed in the kidney tubule, in fetal lung tissue and lung cancer. V1a receptors mediate vasoconstriction, myocardial hypertrophy, platelet aggregation, glycogenolysis, and uterine contraction. V1b receptors mediate corticotrophin (ACTH) release while V2 receptors mediate free water reabsorption and maintain water homeostasis. Due to their involvement in a large spectrum of physiologic processes, antagonists of VP receptors have been developed for the treatment of diseases, such as hyponatremia.
Here, we present an introduction of different subtypes of vasopressin receptors, including the structure, signaling pathways, tissue distribution, functions, and applications.
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