Cat. No. 2598
Chemical Name: (±)-1-[(3R*,4R*)-1-(Cyclooctylmethyl
Biological ActivityPotent 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.
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 / Safety Data Sheet
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.
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.
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.
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Keywords: J 113397, supplier, Potent, selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioid, J113397
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κ-opioid agonist; antinociceptive
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