ONO-2952

Research use only, not for human use.

A novel potent, selective, orally active translocator protein 18 kDa (TSPO/PBR) antagonist with Ki of 0.33-9.3 nM for both rat and human TSPO.

A novel potent, selective, orally active translocator protein 18 kDa (TSPO/PBR) antagonist with Ki of 0.33-9.3 nM for both rat and human TSPO; displays high selectivity over 98 other receptors, transporters, ion channels and enzymes; inhibits both neurosteroid accumulation and noradrenaline release in the brain of rats exposed to acute stress; suppresses conditioned fear stress-induced freezing behavior in rats with an efficacy equivalent to that of diazepam, but without not affect learning and memory.Irritable Bowel Syndrome Phase 2 Clinical.

As for its selectivity for TSPO, ONO-2952 at a concentration of 10 μM showed good selectivity for TSPO against 98 off-targets (<50% inhibition). Determination of ONO-2952 Ki or IC50 values for the remaining 35 targets (50% inhibition at 10 μM) reveal Ki values of less than 1 μM only for 3 receptors, i.e. melatonin 2, progesterone B, and adrenergic α2C. The affinity of ONO-2952 for these receptors is at least 59 times lower than that for TSPO. ONO-2952 Ki value for the GABAA receptor is more than 600 times higher than that for TSPO.

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. Animal Model:Male Sprague Dawley rats (8 weeks old) under conditioned fear stress testDosage: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.

ONO 2952 | ONO2952

Others

TSPO

TSPO

Other Indications

Irritable Bowel Syndrome

895169-20-7

398.862

C22H20ClFN2O2

>98% (HPLC)

In Vitro:?DMSO : 180 mg/mL (451.29 mM)

CC(N([C@H]1C2=CC=C(Cl)C=C2OC)CC3(C4=C1NC5=C4C(F)=CC=C5)CC3)=O

1-[(1S)-1-(4-Chloro-2-methoxyphenyl)-5-fluoro- 1,9-dihydrospiro[b-carboline-4,10 -cyclopropan]-2(3H)-yl]ethanone

(-20℃)

With Ice Pack

≥ 2 years