Vasopressin (AVP) and its receptors play a pivotal role in maintaining body homeostasis under physiological
and pathophysiological conditions. As a consequence, the vasopressin system has emerged as an important target
for both diagnostic and therapeutic applications in a number of medical conditions. Stoichiometric generation of AVP
with copeptin, which is relatively accessible in the blood for measurements, makes copeptin a valuable surrogate of
AVP. In this review, we present the regulation of release of AVP and activation of V1a, V1b, and V2 vasopressin
receptors under physiological and pathological conditions. We make a survey of the role of AVP in: the regulation of
the cardiovascular system; body fluid osmolality; natraemia; endocrine regulation; food intake; metabolism; circadian
rhythmicity, immunological processes; and in the formation of learning, memory, cognition, and emotional and social
behaviours. We also discuss the significance of the inappropriate functioning of the vasopressin system for: the development
of cardiovascular diseases; disturbances of the water-electrolyte balance; energy metabolism; inflammatory
processes; pain; neurogenic stress; memory disorders; depression; anxiety; autism; and schizophrenia. The structure
and biological properties of peptide and non-peptide agonists and antagonists of V1a, V1b and V2 vasopressin receptors
are presented and the potential use of copeptin and the current and likely indications for AVP agonists and antagonists
in the diagnosis and therapeutics of multiple pathological conditions is discussed.
Keywords: Antidiuretic hormone, biomarkers, cardiovascular diseases, neuropeptides, psychiatric disorders, vaptans.
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