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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