(±)-J 113397

Cat. No. 2598

J 113397 C24H37N3O2 [217461-40-0]

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Chemical Name: (±)-1-[(3R*,4R*)-1-(Cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one

Biological Activity

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

M.Wt:
399.57
Formula:
C24H37N3O2
Solubility:
Soluble to 50 mM in DMSO and to 50 mM in ethanol
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
217461-40-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
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Marti et al (2007) The nociceptin/orphanin FQ receptor antagonist J-113397 and L-DOPA additively attenuate experimental Parkinsonism through overinhibition of nigrothalamic pathway. J.Neurosci. 27 1297. PMID: 17287504.

Ozaki et al (2000) In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. Eur.J.Pharmacol. 402 45. PMID: 10940356.

Kawamoto et al (1999) 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). J.Med.Chem. 42 5061. PMID: 10602690.

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Citations are publications that use Tocris products. Selected citations for (±)-J 113397 include:

Wen et al (2011) Pharmacological mechanisms underlying the antinociceptive and tolerance effects of the 6,14-bridged oripavine compound 030418. Acta Pharmacol Sin 32 1215. PMID: 21863064.

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Keywords: J 113397, supplier, Potent, selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioid, J113397, Tocris Bioscience, NOP Receptor Antagonist products

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