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J-113397

Names

[ CAS No. ]:
217461-40-0

[ Name ]:
J-113397

[Synonym ]:
1-[(3R,4R)-1-(Cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one - 1-[(3S,4S)-1-(cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (1:1)
2H-Benzimidazol-2-one, 1-[(3R,4R)-1-(cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl-1,3-dihydro-, compd. with 1-[(3S,4S)-1-(cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (1:1)

Biological Activity

[Description]:

(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a Ki of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC50 value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease

[Target]

Ki: 1.8 nM (human ORL1)[1]


[References]

[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;402(1-2):45-53.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H37N3O2

[ Molecular Weight ]:
399.57

[ Exact Mass ]:
798.577148

Related Compounds