Vasopressin receptor
Encyclopedia
A vasopressin receptor is a cell surface receptor
which binds vasopressin
. The three types of vasopressin receptor are members of the A6 subfamily of G-protein coupled receptors.
, while activation of AVPR2 stimulates adenylate cyclase
. These three receptors for vasopressin have unique tissue distributions. AVPR1A are expressed in vascular smooth muscle cells, hepatocytes, platelets, brain cells, and uterus cells. AVPR1B are expressed in cells of the anterior pituitary and throughout the brain, especially in the pyramidal neurons of the hippocampal CA2 field. AVPR2 are expressed in the kidney tubule, predominantly in the distal convoluted tubule
and collecting ducts, in fetal lung
tissue and lung cancer
, the last two being associated with alternative splicing
. AVPR2 is also expressed in the liver where stimulation releases a variety of clotting factors into the bloodstream. In the kidney, AVPR2's primary function is to respond to arginine vasopressin by stimulating mechanisms that concentrate the urine
and maintain water
homeostasis
in the organism. When the function of AVPR2 is lost, the disease Nephrogenic Diabetes Insipidus
(NDI) results.
s are drugs that block the action that occurs at the vasopressin receptor to treat diseases. The most common disease these are used to treat is hyponatremia
, which causes serious complications for such illnesses as liver cirrhosis and congestive heart failure. Vasopressin receptor antagonists include the new class of "vaptan drugs", including lixivaptan
.
Receptor (biochemistry)
In biochemistry, a receptor is a molecule found on the surface of a cell, which receives specific chemical signals from neighbouring cells or the wider environment within an organism...
which binds vasopressin
Vasopressin
Arginine vasopressin , also known as vasopressin, argipressin or antidiuretic hormone , is a neurohypophysial hormone found in most mammals, including humans. Vasopressin is a peptide hormone that controls the reabsorption of molecules in the tubules of the kidneys by affecting the tissue's...
. The three types of vasopressin receptor are members of the A6 subfamily of G-protein coupled receptors.
Subtypes
Humans express three subtypes: 1A, 1B and 2Receptor | Gene | G protein G protein G proteins are a family of proteins involved in transmitting chemical signals outside the cell, and causing changes inside the cell. They communicate signals from many hormones, neurotransmitters, and other signaling factors. G protein-coupled receptors are transmembrane receptors... |
Functions |
---|---|---|---|
Arginine vasopressin receptor 1A Arginine vasopressin receptor 1A Arginine vasopressin receptor 1A is one of the three major receptor types for arginine vasopressin , and is present throughout the brain, as well as in the periphery in the liver, kidney, and vasculature.Arginine vasopressin receptor 1A is also known as:* V1a vasopressin receptor* antidiuretic... |
AVPR1A | Gq Gq alpha subunit Gq protein or Gq/11 is a heterotrimeric G protein subunit that activates phospholipase C . PLC in turn hydrolyzes Phosphatidylinositol 4,5-bisphosphate to diacyl glycerol and inositol triphosphate signal transduction pathway... |
Vasoconstriction Vasoconstriction Vasoconstriction is the narrowing of the blood vessels resulting from contraction of the muscular wall of the vessels, particularly the large arteries, small arterioles and veins. The process is the opposite of vasodilation, the widening of blood vessels. The process is particularly important in... |
Arginine vasopressin receptor 1B Arginine vasopressin receptor 1B Arginine vasopressin receptor 1B is a protein that acts as receptor for arginine vasopressin. AVPR1B belongs to the subfamily of G-protein coupled receptors... also called Arginine vasopressin receptor 3 |
AVPR1B | Gq | Neural |
Arginine vasopressin receptor 2 Arginine vasopressin receptor 2 Arginine vasopressin receptor 2 is a protein that acts as receptor for arginine vasopressin. AVPR2 belongs to the subfamily of G-protein-coupled receptors... |
AVPR2 | Gs Gs alpha subunit The Gs alpha subunit is a heterotrimeric G protein subunit that activates the cAMP-dependent pathway by activating adenylate cyclase.-Receptors:The G protein-coupled receptors that couple to this kind of G-protein include:... |
Antidiuretic Antidiuretic An antidiuretic is an agent or drug that, administered to an organism, helps control body water balance by reducing urination, opposing diuresis.-Uses:... |
Function
Although all three of these proteins are G-protein coupled receptors (GPCRs), activation of AVPR1A and AVPR1B stimulate phospholipase CPhospholipase C
Phosphoinositide phospholipase C is a family of eukaryotic intracellular enzymes that play an important role in signal transduction processes. In general, this enzyme is denoted as Phospholipase C, although three other families of phospholipase C enzymes have been identified in bacteria and in...
, while activation of AVPR2 stimulates adenylate cyclase
Adenylate cyclase
Adenylate cyclase is part of the G protein signalling cascade, which transmits chemical signals from outside the cell across the membrane to the inside of the cell ....
. These three receptors for vasopressin have unique tissue distributions. AVPR1A are expressed in vascular smooth muscle cells, hepatocytes, platelets, brain cells, and uterus cells. AVPR1B are expressed in cells of the anterior pituitary and throughout the brain, especially in the pyramidal neurons of the hippocampal CA2 field. AVPR2 are expressed in the kidney tubule, predominantly in the distal convoluted tubule
Distal convoluted tubule
The distal convoluted tubule is a portion of kidney nephron between the loop of Henle and the collecting duct system.- Physiology :It is partly responsible for the regulation of potassium, sodium, calcium, and pH...
and collecting ducts, in fetal lung
Lung
The lung is the essential respiration organ in many air-breathing animals, including most tetrapods, a few fish and a few snails. In mammals and the more complex life forms, the two lungs are located near the backbone on either side of the heart...
tissue and lung cancer
Lung cancer
Lung cancer is a disease characterized by uncontrolled cell growth in tissues of the lung. If left untreated, this growth can spread beyond the lung in a process called metastasis into nearby tissue and, eventually, into other parts of the body. Most cancers that start in lung, known as primary...
, the last two being associated with alternative splicing
Alternative splicing
Alternative splicing is a process by which the exons of the RNA produced by transcription of a gene are reconnected in multiple ways during RNA splicing...
. AVPR2 is also expressed in the liver where stimulation releases a variety of clotting factors into the bloodstream. In the kidney, AVPR2's primary function is to respond to arginine vasopressin by stimulating mechanisms that concentrate the urine
Urine
Urine is a typically sterile liquid by-product of the body that is secreted by the kidneys through a process called urination and excreted through the urethra. Cellular metabolism generates numerous by-products, many rich in nitrogen, that require elimination from the bloodstream...
and maintain water
Water
Water is a chemical substance with the chemical formula H2O. A water molecule contains one oxygen and two hydrogen atoms connected by covalent bonds. Water is a liquid at ambient conditions, but it often co-exists on Earth with its solid state, ice, and gaseous state . Water also exists in a...
homeostasis
Homeostasis
Homeostasis is the property of a system that regulates its internal environment and tends to maintain a stable, constant condition of properties like temperature or pH...
in the organism. When the function of AVPR2 is lost, the disease Nephrogenic Diabetes Insipidus
Nephrogenic diabetes insipidus
Nephrogenic diabetes insipidus is a form of diabetes insipidus due primarily to pathology of the kidney. This is in contrast to central/neurogenic diabetes insipidus, which is caused by insufficient levels of antidiuretic hormone /Argenine Vasopressin...
(NDI) results.
Role in Disease Treatment
Vasopressin receptor antagonistVasopressin receptor antagonist
A vasopressin receptor antagonist is an agent which interferes with action at the vasopressin receptors. They can be used in the treatment of hyponatremia, especially in patients with congestive heart failure or liver cirrhosis.-Tetracyclines:...
s are drugs that block the action that occurs at the vasopressin receptor to treat diseases. The most common disease these are used to treat is hyponatremia
Hyponatremia
Hyponatremia is an electrolyte disturbance in which the sodium concentration in the serum is lower than normal. In the vast majority of cases, hyponatremia occurs as a result of excess body water diluting the serum sodium and is not due to sodium deficiency. Sodium is the dominant extracellular...
, which causes serious complications for such illnesses as liver cirrhosis and congestive heart failure. Vasopressin receptor antagonists include the new class of "vaptan drugs", including lixivaptan
Lixivaptan
Lixivaptan is a phase III pharmaceutical being developed by Cardiokine, Inc., a specialty pharmaceutical company based in Philadelphia, PA, focused on the development of pharmaceuticals for the treatment and prevention of cardiovascular diseases...
.