ONO-2952 is a potent, selective and orally active translocator protein 18 kDa (TSPO) antagonist with K i 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 In Vitro As for its selectivity for TSPO, ONO-2952 at a concentration of 10 μM showed good selectivity for TSPO against 98 off-targets ( 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 . ONO-2952 inhibits both neurosteroid accumulation and noradrenaline release in the brain of rats exposed to acute stress . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague Dawley rats (8 weeks old) under conditioned fear stress test 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. Form:Solid IC50& Target:Ki: 0.33-9.30 nM (Rat and human TSPO)
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ONO-2952
CAS number：895169-20-7 molecular formula：C22H20ClFN2O2
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| Chinese alias | - | ||
| English alias | ONO-2952 | ONO 2952 | UNII-ZH8CPX4YNB | 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)- | MS-26749 | ZH8CPX4YNB | 1-((1S)-1-(4-CHLORO-2-METHOXYPHENYL)-5-FLUORO-1,9-DI | ||
| CAS number | 895169-20-7 | molecular formula | C22H20ClFN2O2 |
| molecular weight | 398.86 g/mol | Exact mass | ≥99% |
| PSA | 45.300 Ų | logp | 4.1 |
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