Effect of YM471, a nonpeptide AVP receptor antagonist, on human coronary artery smooth muscle cells

Vasopressin and Its Analogues: From Natural Hormones to Multitasking Peptides

“…They include the following: increase in cortisol concentration through the induction of corticotropic axis stimulation [ 52 ], insulin secretion, release of coagulant factors [ 45 ], regulation of lipid metabolism [ 56 ], stimulation of water reabsorption, regulation of glucose mechanism, platelet aggregation, modulation of neuronal functions [ 54 ], growth of surface placental leucine aminopeptidase (P-LAP; enzyme crucial to maintain pregnancy) level [ 67 ], rise of plasma osmolality, regulation of blood pressure and volume [ 66 ] and reduction in arrhythmias and tachycardia [ 26 ]. AVP has also been shown to affect modulation of fear and memory [ 27 ], maintain cardiovascular homeostasis through vascular smooth muscle cell contraction [ 68 ], regulate pancreatic islet function [ 46 ], reduce hemorrhage [ 69 ] and, together with angiotensin II, preserve fluid and electrolyte balance [ 70 ]. Its expression in CNS has an impact on a variety of brain functions such as social interaction and recognition, aggression, maternal behavior, pair-bonding behavior and depression [ 21 ].…”

“…Such non-peptide agonists and antagonists of AVP receptors are presented in Figure 4 . Compound 1 had a high affinity to human V1a receptor (hV1a) and potently inhibited AVP-induced physiological responses of human coronary artery smooth muscle cells (CASMC) [ 68 ]. Compounds 2 and 3 showed high binding efficiencies to the hV1a receptor [ 78 ] and a similar chemical structure based on 4,5-diphenyl-1,2,4,-triazole moiety.…”