Arginine-vasopressin receptor

Williams, B., P. Tsai, and R.W. Schrier. 1992. Glucose-induced downregulation of angiotensin II and arginine vasopressin receptors in cultured rat aortic vascular smooth muscle cells. Role of protein kinase C. J. Clin. Invest. 90 1992-1999. 

Desmopressin, used to improve platelet function by activating arginine vasopressin receptor lA. 

Arginine vasopressin receptor 2 (AVPR2) Xq28 W71 truncation and many SNPs... 

Hensen J, Haenelt M, Gross P. Water retention after oral chlorpropamide is associated with an increase in renal papillary arginine vasopressin receptors. Eur J Endocrinol 1995 132 459-464. 

Kim SJ, Young LJ, Gonen D, Veenstra-VanderWeele J, Courchesne R, Courchesne E, Lord C, Leventhal BL, Cook EH, Jr., Insel TR (2002) Transmission disequilibrium testing of arginine vasopressin receptor lA (AVPRIA) polymorphisms in autism. Mol Psychiatry 7 503-507. 

There are three subtypes of arginine vasopressin receptor, Vja., Vib, and V2. The V2 receptor is mainly situated in the kidney and is important in free water reabsorption [41 ]. The ViB receptor mediates adreno-coticotropin release in the anterior pituitary. The Via receptor has multiple... 

Logically, ADH receptor antagonists, and ADH synthesis and release inhibitors can be effective aquaretics. ADH, 8-arginine vasopressin [113-79-17, is synthesized in the hypothalamus of the brain, and is transported through the supraopticohypophyseal tract to the posterior pituitary where it is stored. Upon sensing an increase of plasma osmolaUty by brain osmoreceptors or a decrease of blood volume or blood pressure detected by the baroreceptors and volume receptors, ADH is released into the blood circulation it activates vasopressin receptors in blood vessels to raise blood pressure, and vasopressin V2 receptors of the nephrons of the kidney to retain water and electrolytes to expand the blood volume. 

X-linked nephrogenic diabetes insipidus (NDI) is caused by mutations in the gene for the vasopressin V2 receptor leading to an insensitivity of the kidney for the antidiuretic hormone arginine vasopressin (AVP). The main symptom of the disease is diuresis, i.e., the production of a large amount of diluted urine. Due to the massive loss of water, the patients suffer from thirst and are in danger of dehydration. The disease usually becomes evident shortly after birth. 

A vasopressin V2 receptor antagonist, lixivaptan, is currently being developed (Phase 11) for the treatment of hyponatremia. This agent blocks the effect of the antidiuretic hormone arginine-vasopressin. 

Antagonists of the vasoconstrictor action of vasopressin are also available. The peptide antagonist (l-[B-mercapto-B,B-cyclopentamethylenepropionic acid]-2-[0 -methyl]tyrosine) arginine vasopressin also has antioxytocic activity but does not antagonize the antidiuretic action of vasopressin. Recently, nonpeptide, orally active Via receptor antagonists have been discovered, an example being relcovaptan. 

Arginine vasopressin Agonist of vasopressin (and V2) receptors Vasoconstriction Vasodilatory shock... 

Desmopressin f/V-deamino-8-D-arginine vasopressin, dDAVP) is a longer acting analogue of vasopressin. It has very little vasoactive effect but is antidiuretic by an action on vasopressin V2 receptors in the renal tubule and is used to treat central diabetes insipidus and nocturnal enuresis. 

Figure 18.4. Endocrine-immune inter-relationship following acute stress. In response to stress, corticotrophin releasing factor (CRF) and arginine vasopressin (AVP) are secreted from the hypothalamus causing the release of adrenocortico-trophic hormone (ACTH) from the pituitary. ACTH interacts with receptors on adrenocortical cells and cortisol is released from the adrenal glands. Release of cortisol into the circulation has a number of effects, including elevation of blood glucose. The negative feedback of cortisol on the hypothalamus, pituitary and immune system remains unaffected in acute stress - the release of CRF, AVP and immunotransmitters is still inhibited, preventing the continual activation of the...

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