Description
(±)-J 113397 is a potent and selective non-peptidyl antagonist of ORL1 receptor, with a Ki value of 1.8 nM for cloned human ORL1 . The ORL1 receptor is a G protein-coupled. It is structurally related to the opioid receptors. The heptadecapeptide nociceptin/orphanin FQ is the endogenous ligand . In CHO-ORL1 cells, nociceptinr/orphanin FQ dose-dependently suppressed the accumulation of cyclic AMP stimulated by forskolin with an EC value of 0.22 ± 0.011 nM. Treatment with J-113397 at increasing concentration shifted the concentration-response curve of nociceptinr/orphanin FQ to the right. Data indicated that J-113397 inhibited the interaction between nociceptinr/orphanin FQ and ORL1 in a competitive manner . In a tail-flick test, an i.c.v. injection of nociceptinr/orphanin FQ at 0.01-1 nmol or saline was given to mice. I.c.v. injection of saline did not obviously change the latency of tail-flick. Nociceptinr/orphanin FQ at doses of more than 0.1 nmol shortened the latency. At the high concentration, the effect of nociceptinr/orphanin FQ reached a maximal decrease at 15 min after the injection of J-113397. The effect of nociceptinr/orphanin FQ lasted for more than 60 min. J-113397 inhibited the shortening of mouse tail-flick latency induced by nociceptinr/orphanin FQ dose-dependently. J-113397 at 30 mg/kg completely reversed the hyperalgesia elicited by nociceptinr/orphanin FQ .
Product information
CAS Number: 217461-40-0
Molecular Weight: 399.57
Formula: C24H37N3O2
Chemical Name: 1-[(3R,4R)-1-(cyclooctylmethyl)-3-(hydroxymethyl)piperidin-4-yl]-3-ethyl-2,3-dihydro-1H-1,3-benzodiazol-2-one
Smiles: CCN1C(=O)N([C@@H]2CCN(C[C@H]2CO)CC2CCCCCCC2)C2=CC=CC=C12
InChiKey: MBGVUMXBUGIIBQ-LEWJYISDSA-N
InChi: InChI=1S/C24H37N3O2/c1-2-26-22-12-8-9-13-23(22)27(24(26)29)21-14-15-25(17-20(21)18-28)16-19-10-6-4-3-5-7-11-19/h8-9,12-13,19-21,28H,2-7,10-11,14-18H2,1H3/t20-,21+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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