Vasopressin receptor

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The actions of vasopressin are mediated by stimulation of tissue-specific G protein-coupled receptors (GPCRs) called vasopressin receptors that are classified into the V1 (V1A), V2, and V3 (V1B) receptor subtypes.[1] These three subtypes differ in localization, function and signal transduction mechanisms.[2]

Subtypes

There are three subtypes of vasopressin receptor: V1A (V1), V1B (V3) and V2.[1]

Subtype (symbol) Signaling pathways Location Function
gene receptor
IUPHAR
 alternate
AVPR1A
 V1A V1 G protein-coupled, phosphatidylinositol/calcium vascular smooth muscle, platelet, hepatocytes, myometrium vasoconstriction, myocardial hypertrophy, platelet aggregation, glycogenolysis, uterine contraction
AVPR1B
 V1B V3 G protein-coupled, phosphatidylinositol/calcium anterior pituitary gland releases ACTH, prolactin, endorphins
AVPR2
 V2 V2 Adenylyl cyclase/cAMP basolateral membrane of collecting duct, vascular endothelium and vascular smooth muscle cell insertion of AQP-2 water channels into apical membrane, induction of AQP-2 synthesis, releases von Willebrand factor and factor VIII, vasodilation

V1 receptor

Main article: Vasopressin receptor 1A

V1 receptors (V1Rs) are found in high density on

blood vessels, and renal medulla.[1]

V1R is present on

platelets, which upon stimulation induces an increase in intracellular calcium, facilitating thrombosis. Studies have indicated that due to polymorphism of platelet V1R there is significant heterogeneity in the aggregation response of normal human platelets to vasopressin.[1]

V1Rs are found in

afferent arteriole.[1]

V2 receptor

Main article: Vasopressin receptor 2

V2 receptor (V2R) differs from V1R primarily in the number of sites susceptible to N-linked glycosylation; the V1R has sites at both the amino-terminus and at the extracellular loop, whereas the V2R has a single site at the extracellular amino-terminus.[1]

The well known

principal cells, increasing water reabsorption.[1]

V3 receptor

Main article: Vasopressin receptor 1B

The human V3 receptor (V3R, previously known as V1BR) is a G-protein-coupled

G-proteins, depending on the level of receptor expression.[1]

Function

Although all three of these proteins are

Nephrogenic Diabetes Insipidus (NDI) results.[4]

Antagonists

congestive heart failure (CHF) and cirrhosis.[2]

Somatostatin is a competitive inhibitor. [5]

Normally, when osmolality falls below its set point, plasma vasopressin levels become undetectable, and an aquaresis results. In

CHF, impaired delivery of solute to the diluting sites or diminished glomerular filtration rate causes impairment of maximal water-excretory capacity, resulting in persistence of vasopressin release leading to water retention.[2]

Vasopressin receptor antagonists include the new class of "vaptan drugs" such as conivaptan, tolvaptan, mozavaptan, lixivaptan, satavaptan etc.

References

  1. ^
    PMID 14624682
    .
  2. ^
    PMID 16672911
    .
  3. PMID 27499021
    .
  4. S2CID 20462680
    .
  5. ^ Inhibition by somatostatin of the vasopressin-stimulated adenylate cyclase in a kidney-derived line of cells grown in defined medium. FEBS Letters. https://doi.org/10.1016/0014-5793(84)80304-X

External links

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