vasopressin receptor 1a

Tolvaptan (OPC-41061) is an orally active, selective, competitive vasopressin receptor 2 (V2R) antagonist (IC50 = 1.28 μM) that inhibits AVP-induced platelet aggregation. Tolvaptan is used in studies of hyponatremia.

Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors. It is used for the research of autism.

L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.

Felypressin (Octapressin) is a synthetic analog of LYPRESSIN with a PHENYLALANINE substitution at residue 2. Felypressin is a vasoconstrictor with reduced antidiuretic activity.

Desmopressin (DDAVP)(DDAVP) is the synthetic analogue of the antidiuretic hormone arginine vasopressin.Vasopressin Receptor The antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin works by limiting the amount of water that is eliminated in the urine. Desmopressin binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates release of von Willebrand factor from endothelial cells by acting on the V2 receptor.

Desmopressin acetate (DDAVP) is the synthetic analog of the antidiuretic hormone arginine vasopressin. Vasopressin Receptor The antidiuretic properties of desmopressin have led to its use in polyuric conditions including primary nocturnal enuresis, nocturia, and diabetes insipidus. Desmopressin acetate (16679-58-6 free base) works by limiting the amount of water that is eliminated in the urine. Desmopressin acetate (16679-58-6 free base) binds to V2 receptors in renal collecting ducts, increasing water reabsorption. It also stimulates the release of von Willebrand factor from endothelial cells by acting on the V2 receptor.

Conivaptan hydrochloride (Vaprisol) is an orally active vasopressin V2 and V1A receptor antagonist, used in the therapy of hypervolemic hyponatremia and euvolemic.

SRX246 has no interaction at V1b and V2 receptors. SRX246 shows negligible binding at 64 other receptors classes, including 35 G-proteincoupled receptors. SRX246 is a potent and CNS-penetrant vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V

TC OT 39 is an oxytocin analog and selective agonist of OXTR (oxytocin receptor) (EC50=180 nM), also acting as a V1aR (vasopressin 1a receptor) antagonist. It mimics oxytocin-induced scratching in mouse models.

WAY-267464 is a non-peptide oxytocin receptor agonist that impairs social cognition in rats by acting as a vasopressin 1A receptor antagonist, making it useful for studying psychiatric disorders.

Val9-Oxytocin, an Oxytocin analog where Gly9 is substituted with Val9 [1], functions as a complete antagonist of the vasopressin (V1a) receptor.

'(D-Arg8)-Inotocin is a potent, selective, and competitive antagonist of the vasopressin receptor (V 1a R), exhibiting a binding affinity (K i) of 1.3 nM. It demonstrates over 3000-fold selectivity for the human V1aR compared to the OTR, V1bR, and V2R subtypes [1].'