Sistema FMUSP-HC: Faculdade de Medicina da Universidade de São Paulo (FMUSP) e Hospital das Clínicas da FMUSPGIRARDI, A. C. C.CARRARO-LACROIX, L. R.MORAIS, C. A. C. De2023-02-092023-02-092013Girardi, A. C. C.; Carraro-Lacroix, L. R.; De Morais, C. A. C.. The aquaretic effect of vasopressin V2 receptor antagonists. In: . DIURETICS: PHARMACOLOGY, THERAPEUTIC USES AND ADVERSE SIDE EFFECTS: NOVA SCIENCE PUBLISHERS, INC., 2013. p.1-37.9781628082548https://observatorio.fm.usp.br/handle/OPI/51308The control of body osmolality is crucial for the maintenance of normal cell volume and can be accomplished by controlling water balance. The kidneys represent the major route for the elimination of water from the body, and water balance can be achieved without affecting the renal excretion of other electrolytes. In the kidney, the hormone arginine vasopressin (AVP) remarkably increases the permeability of the distal nephron to water by increasing the density of the water channel aquaporin 2 (AQP2). More specifically, AVP binds to its V2 receptor located at the basolateral membrane of the collecting duct cells, activates the cAMP/PKA signal transduction pathway and induces translocation of the AQP2 from cytoplasmic storage vesicles to the apical membrane. The development of bioavailable AVP antagonists with a high affinity for V2 receptors represents a promising approach for the treatment of hypervolemic and euvolemic hyponatremia due to its unique aquaretic effect. The goals of this chapter are to describe the physiology of vasopressin and the role of this hormone in water balance and to discuss the pharmacodynamics and pharmacokinetics of VAPTANS (nonpeptide vasopressin receptor antagonists), as well as their current and predictable therapeutic uses, based on recent data from pre-clinical studies and clinical trials. © 2013 Nova Science Publishers, Inc.engrestrictedAccessbookPartCopyright NOVA SCIENCE PUBLISHERS, INC.