| Identification | Back Directory | [Name]
Ethanone, 1-[(1'S)-1'-(4-chloro-2-methoxyphenyl)-5'-fluoro-1',2',3',9'-tetrahydrospiro[cyclopropane-1,4'-[4H]pyrido[3,4-b]indol]-2'-yl]- | [CAS]
895169-20-7 | [Synonyms]
ONO-2952
ONO2952,ONO 2952
Ethanone, 1-[(1'S)-1'-(4-chloro-2-methoxyphenyl)-5'-fluoro-1',2',3',9'-tetrahydrospiro[cyclopropane-1,4'-[4H]pyrido[3,4-b]indol]-2'-yl]- | [Molecular Formula]
C22H20ClFN2O2 | [MDL Number]
MFCD32661907 | [MOL File]
895169-20-7.mol | [Molecular Weight]
398.86 |
| Hazard Information | Back Directory | [Uses]
ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with Ki of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment[1][2]. | [in vivo]
ONO-2952 (0.03-3 mg/kg; oral administration; male Sprague Dawley rats) treatment dose-dependently suppresses restraint stress-induced defecation in rats with brain TSPO occupancy of more than 50%. ONO-2952 also suppresses conditioned fear stress-induced freezing behavior in rats[1].
ONO-2952 inhibits both neurosteroid accumulation and noradrenaline release in the brain of rats exposed to acute stress[1]. | Animal Model: | Male Sprague Dawley rats (8 weeks old) under conditioned fear stress test[1] | | Dosage: | 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg | | Administration: | Oral administration | | Result: | Dose-dependently suppressed restraint stress-induced defecation in rats. And suppressed conditioned fear stress-induced freezing behavior in rats.
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| [References]
[1] Mitsui K, et al. Anti-stress effects of ONO-2952, a novel translocator protein 18 kDa antagonist, in rats. Neuropharmacology. 2015 Dec;99:51-66. DOI:10.1016/j.neuropharm.2015.07.011
[2] Whitehead WE, et al. Randomised clinical trial: exploratory phase 2 study of ONO-2952 in diarrhoea-predominant irritable bowel syndrome. Aliment Pharmacol Ther. 2017 Jan;45(1):14-26. DOI:10.1111/apt.13839 |
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