Vasopressin Type 2 Receptor Agonists and Antagonists

Regulation of water homeostasis is of vital importance for all terrestrial organisms. In most mammals, the maintenance of water balance is strictly dependent on water excretion in the kidney, which is under the control of the antidiuretic hormone arginine vasopressin (AVP). In the kidney, AVP binds to the vasopressin type 2 receptor (V2R). The alteration of water balance and consequent disorders are closely correlated to the fine regulation of the vasopressin-aquaporin 2 (AQP2) axis in the last tract of the renal tubule, the collecting duct. Over the last 20years and currently, the vasopressin—AQP2 axis, via the V2R bridge, was been and is still today the hottest therapeutic target investigated for the treatment of water balance disorders. Therefore, in the last years, significant progress has been made in the discovery and development of vasopressin type 2 receptor (V2R) agonists and antagonists. In this chapter the recent insights on V2R agonists, antagonists and biased agonists are reported. In addition , new approaches and recent advances for the treatment of water balance disorders are discussed.