Vasopressin/Oxytocin GPCR Family Subtypes and Products

What Are Vasopressin/Oxytocin Receptors?

Vasopressin and oxytocin receptors are a family of G protein-coupled receptors (GPCRs) found all throughout the brain and peripheral tissue, contributing to a wide range of biological functions. This family is comprised of four receptor subtypes: OT, V1A, V1B, and V2. Peripheral roles for these receptors are more established, such as uterine muscle contraction and the prevention of bodily fluid loss. V2 agonists are used to treat bleeding disorder. In addition, they also play a large role in a variety of social and psychological behaviors, such as attachment, generosity, bonding, and maternal behavior.

Vasopressin/Oxytocin Receptor Information

Clickable Text Interaction

OT

V1A

V1B

V2

Oxytocin (OT) is a member of the neurohypophyseal hormone family. OT receptors are found in uterine smooth muscle, myoepithelial cells in the mammary gland, and in the pituitary. OT stimulates contraction of uterine smooth muscle during labor and stimulates milk secretion in response to suckling. It has been postulated that OT may also facilitate social and bonding behaviors related to the reproduction and care of offspring. Further studies of the OT receptor are essential in gaining a better understanding of the mechanism and in vivo regulation of uterine function.

V1A, a G protein coupled receptor, also called arginine vasopressin 1A (AVPR1A), is a receptor for neurohypophyseal peptide [Arg8]-vasopressin. V1A has shown to be highly expressed in the posterior pituitary gland, where it plays an essential role in controlling the water content of the body by acting on the kidney to increase water and sodium absorption. It is also abundant in the periphery in vascular smooth muscle, myometrium and the bladder, where it also acts to mediate contraction. Other functions include glycogen breakdown in the liver, inducing platelet activation, and triggering the release of corticotrophin from the anterior pituitary gland. Vasopressin is used clinically to treat diabetes insipidus. V1a receptor signals through phosphatidylinositol hydrolysis to mobilize intracellular Ca2+. Studies have shown V1A receptor antagonists to selectively block aggressive behavior in hamsters. Repeat variations in V1A has also been associated with the risk of autism, level of musical cognition, and level of altruism.

V1B, a G protein coupled receptor, also called arginine vasopressin 1B (AVPR1B), is a receptor for neurohypophyseal peptide [Arg8]-vasopressin. V1B receptor was previously known as vasopressin 3 receptor or antidiuretic hormone receptor 1b. V1B has been shown to be expressed highly in the anterior pituitary gland, where it stimulates corticotrophin release, and also in low levels in the brain and adrenal glands. V1b receptor signals through phosphatidylinositol hydrolysis to mobilize intracellular Ca2+. A single nucleotide polymorphism in VIB receptor has been associated with susceptibility to depression in humans. Highly selective peptide and nonpeptide vasopressin receptor antagonists have been developed and pharmacological studies have provided evidence for its role in stress related behavior and disorders including anxiety disorders and depression, while deletion of the V1B gene in mice has been shown to greatly reduce aggression. In addition, knockout of V1B gene has shown reduction of vasopressin-stimulated insulin release from islet cells is mediated via V1b receptors.

V2, a G protein coupled receptor, also called arginine vasopressin receptor 2 (AVPR2), is a receptor for neurohypophyseal peptide [Arg8]-vasopressin. It is expressed in the kidney tubule, mainly in the membrane of cells of the distal convoluted tubule and collecting ducts, in fetal lung tissue and lung cancer. In the kidney, V2 receptor responds to vasopressin and activates mechanisms that concentrate urine and maintain water homeostasis in the body. Loss of function of the V2 receptor results in nephrogenic diabetes insipidus. The primary transduction mechanism is via adenylate cyclase stimulation to raise intracellular cAMP levels. Selective antagonists for V2 can be used to treat hyponatremia.

Vasopressin/Oxytocin Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
Vasopressin/OxytocinOThumanCHO-K1C1299-1DC1299-1MC1299-1
OTrabbitHEK293TCb1299DCb1299MCb1299
OTrabbitHEK293TCb1299LDCb1299LMCb1299L
V1AhumanCHO-K1C1042-1DC1042-1MC1042-1
V1ArabbitHEK293TCb1042DCb1042MCb1042
V1BhumanCHO-K1C1043-1DC1043-1MC1043-1
V1BrabbitHEK293TCb1043DCb1043MCb1043
V1BrabbitHEK293TCb1043LDCb1043LMCb1043L
V2humanCHO-K1C1044-1DC1044-1MC1044-1
V2rabbitHEK293TCb1044DCb1044MCb1044
V2rabbitHEK293TCb1044LDCb1044LMCb1044L
V2dogCHO-K1Cd1044-1DCd1044-1MCd1044-1