| Bioactivity | J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors[1]. |
| Invitro | J-113397 (0-500 nM) inhibits NociceptinNociceptin/orphanin FQ (HY-P0183)-stimulated [35S]GTPγS binding to CHO cells expressing ORL1 (CHO-ORL1) but had no effect on [35S]GTPγS binding by itself[1]. Cell Viability Assay[1] Cell Line: |
| In Vivo | J-113397 (0-30 mg/kg; subcutaneously (s.c.); once) dose-dependently inhibits hyperalgesia elicited by intracerebroventricular (i.c.v.) administration of NociceptinNociceptin/orphanin FQ (HY-P0183) in a tail-flick test with mice[1]. Animal Model: |
| Name | J-113397 |
| CAS | 256640-45-6 |
| Formula | C24H37N3O2 |
| Molar Mass | 399.57 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ozaki S, et al. In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. Eur J Pharmacol. 2000 Aug 18;402(1-2):45-53. |