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ONO-2952 

Cat. No.: HY-111191
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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.

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ONO-2952 Chemical Structure

ONO-2952 Chemical Structure

CAS No. : 895169-20-7

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Description

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].

IC50 & Target

Ki: 0.33-9.30 nM (Rat and human TSPO)[1]

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 (<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[1].

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.
Clinical Trial
Molecular Weight

398.86

Formula

C₂₂H₂₀ClFN₂O₂

CAS No.

895169-20-7

SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ONO-2952ONO2952ONO 2952OthersTSPOCNSneurosteroidnoradrenalineanti-stressirritablebowelsyndromeamnesicInhibitorinhibitorinhibit

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ONO-2952
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HY-111191
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