OPC 21268
Chemical Name: N-[3-[4-[[4-(3,4-Dihydro-2-oxo-1(2H)quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide
Purity: ≥98%
Biological Activity
OPC 21268 is a nonpeptide vasopressin V1 receptor antagonist. Displays greater affinity for rat V1 than human V1 (Ki values are 25 and 8800 nM respectively). Exhibits 1000-fold selectivity for V1 receptors over V2 receptors. Orally active.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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OPC-21268, an orally effective, nonpeptide vasopressin V1 receptor antagonist.
Yamamura et al.
Science, 1991;252:572 -
Effects of OPC-21268, an orally effective vasopressin V1 receptor antagonist in humans.
Imaizumi et al.
Hypertension, 1992;20:54 -
A molecular model of agonist and nonpeptide antagonist binding to the human V1 vascular vasopressin receptor.
Thibonnier et al.
J.Pharmacol.Exp.Ther., 2000;294:195
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Citations for OPC 21268
The citations listed below are publications that use Tocris products. Selected citations for OPC 21268 include:
3 Citations: Showing 1 - 3
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Evidence for a Prehypertensive Water Dysregulation Affecting the Development of Hypertension: Results of Very Early Treatment of Vasopressin V1 and V2 Antagonism in Spontaneously Hypertensive Rats.
Authors: Gallia Et al.
Front Cardiovasc Med 2022;9:897244
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Reduced VIP Expression Affects Circadian Clock Function in VIP-IRES-CRE Mice (JAX 010908).
Authors: Harshida Et al.
J Biol Rhythms 2020;35:340-352
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Asymmetric vasopressin signaling spatially organizes the master circadian clock.
Authors: Amita Et al.
J Comp Neurol 2018;526:2048-2067
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