(±)-J 113397
Chemical Name: (±)-1-[(3R*,4R*)-1-(Cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
Purity: ≥98%
Biological Activity
(±)-J 113397 is a potent and selective NOP receptor antagonist (IC50 values are 2.3, 1400, 2200 and > 10000 nM for NOP, κ, μ and δ-opioid receptors respectively). Inhibits nociceptin/orphanin FQ-induced hyperalgesia in the mouse tail-flick test.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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Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397).
Kawamoto et al.
J.Med.Chem., 1999;42:5061 -
In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist.
Ozaki et al.
Eur.J.Pharmacol., 2000;402:45 -
The nociceptin/orphanin FQ receptor antagonist J-113397 and L-DOPA additively attenuate experimental Parkinsonism through overinhibition of nigrothalamic pathway.
Marti et al.
J.Neurosci., 2007;27:1297
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Citation for (±)-J 113397
The citations listed below are publications that use Tocris products. Selected citations for (±)-J 113397 include:
1 Citation: Showing 1 - 1
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Pharmacological mechanisms underlying the antinociceptive and tolerance effects of the 6,14-bridged oripavine compound 030418.
Authors: Wen Et al.
Acta Pharmacol Sin 2011;32:1215
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