A nonpeptide antagonist of vasopressin V1 receptors
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OPC 21268

Item No. 27226

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide
CAS Number
131631-89-5
Molecular Formula
C26H31N3O4
Formula Weight
449.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 200 µg/mlEthanol: Slightly soluble
λmax
249 nm
SMILES
O=C1CCC2=CC=CC=C2N1C3CCN(C(C4=CC=C(OCCCNC(C)=O)C=C4)=O)CC3
InChi Code
InChI=1S/C26H31N3O4/c1-19(30)27-15-4-18-33-23-10-7-21(8-11-23)26(32)28-16-13-22(14-17-28)29-24-6-3-2-5-20(24)9-12-25(29)31/h2-3,5-8,10-11,22H,4,9,12-18H2,1H3,(H,27,30)
InChi Key
KSNUCNRMDYJBKT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $169

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    10 mg

    $303

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    25 mg

    $667

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    Product Description

    OPC 21268 is a nonpeptide antagonist of vasopressin V1 receptors (IC50 = 0.4 µM in rat liver membranes).1 It is selective for V1 over V2 receptors (IC50 = >100 µM in kidney membranes). It is also selective for rat over human V1 receptors (Kis = 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; Item No. 24154) in pithed rats and arginine vasopressin-induced vasoconstriction in conscious rats (ID50 = 2 mg/kg).2 It induces hypotension in aged spontaneously hypertensive rats (SHRs) and stroke-prone SHRs when administered at a dose of 3 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Thibonnier, M., Coles, P., Conarty, D.M., et al. A molecular model of agonist and nonpeptide antagonist binding to the human V1 vascular vasopressin receptor. J. Pharmacol. Exp. Ther. 4(1), 195-203 (2000).

    2. Yamamura, Y., Ogawa, H., Chihara, T., et al. OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist. Science 252(5005), 572-574 (1991).

    3. Yamada, Y., Yamamura, Y., Chihara, T., et al. OPC-21268, a vasopressin V1 antagonist, produces hypotension in spontaneously hypertensive rats. Hypertension 23(2), 200-204 (1994).