131631-89-5

OPC 21268 is a nonpeptide antagonist of vasopressin V₁ receptors (IC₅₀ = 0.4 μM in rat liver membranes). It is selective for V₁ over V₂ receptors (IC₅₀ = >100 μM in kidney membranes). It is also selective for rat over human V₁ receptors (K_is = 25 and 8,800 nM, respectively), which can be partially attributed to the alanine residue at position 337 of the rat sequence, instead of a glycine residue in the human sequence, with differences at positions 224, 310, and 324 also contributing. OPC 21268 (0.03-1 mg/kg, i.v.) inhibits pressor responses induced by arginine vasopressin (argipressin; ) in pithed rats and arginine vasopressin-induced vasoconstriction in conscious rats (ID₅₀ = 2 mg/kg). It induces hypotension in aged spontaneously hypertensive rats (SHRs) and stroke-prone SHRs when administered at a dose of 3 mg/kg.

OPC 21268 is a nonpeptide AVP (Vasopressin) Receptor V antagonist.

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[2] YOSHITAKA YAMAMURA. OPC-21268, an Orally Effective, Nonpeptide Vasopressin V1 Receptor Antagonist[J]. Science, 1991, 252 5005. DOI: 10.1126/science.1850553
[3] Y YAMADA. OPC-21268, a vasopressin V1 antagonist, produces hypotension in spontaneously hypertensive rats.[J]. Hypertension, 1994, 23 2: 200-204. DOI: 10.1161/01.hyp.23.2.200