Chemical Name: (±)-1-[(3R*,4R*)-1-(Cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
19.98
50
ethanol
19.98
50
Preparing Stock Solutions
The following data is based on the product molecular weight 399.57. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.5 mL
12.51 mL
25.03 mL
5 mM
0.5 mL
2.5 mL
5.01 mL
10 mM
0.25 mL
1.25 mL
2.5 mL
50 mM
0.05 mL
0.25 mL
0.5 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Kawamotoet 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
Ozakiet 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
Martiet 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