| Cas No.: | 1802661-73-9 |
| Chemical Name: | 1-(cyclopropylmethyl)-5-fluoro-4-methyl-N-[5-(1-methyl-1H-imidazol-4-yl)-2-pyridinyl]-1H-benzimidazol-6-amine |
| Synonyms: | ONO-8590580,ONO 8590580,ONO8590580 |
| SMILES: | C1N(CC2CC2)C2=CC(NC3=NC=C(C4=CN(C)C=N4)C=C3)=C(F)C(C)=C2N=1 |
| Formula: | C21H21FN6 |
| M.Wt: | 376.44 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | ONO-8590580 is a GABAA α5 negative allosteric modulator. |
| Target: | GABAA α5[1]. |
| In Vivo: | The effect of ONO-8590580 on the MK-801/scopolamine-induced cognitive deficit in the 8-arm radial maze test is investigated. Doses of MK-801 and scopolamine for this test are 0.075 mg/kg (i.p.) and 0.2 mg/kg (i.p.) respectively. ONO-8590580 (20 mg/kg, p.o.) significantly decreases the number of errors and total latency compared to the control. The present study in which ONO-8590580 but not donepezil significantly decreases the number of errors may suggest that ONO-8590580 could be more potent for the treatment of AD patients. The data showing that ONO-8590580 has not anxiogenic-like or proconvulsant effects are in agreement with the behavioral phenotype of α5-/- mice[1]. |
| Animal Administration: | Rats[1] Male Sprague-Dawley rats are used. ONO-8590580 is orally administered 1 h before sacrifice. [3H]-Ro15-4513 (1.11 MBq/kg) is administered via the tail vein (1 mL/kg) 10 min before sacrifice. Rats (n=12 in each group) are given either vehicle, ONO-8590580 (20 mg/kg, p.o.), or as a positive control, the GABAA nonselective NAM FG-7142 (15 mg/kg, i.p.). After 1 h, rats are placed in the elevated plus maze for 5 min. Light intensity in the open arms is set at 20 lx. A video camera fitted with a polarizing lens is mounted above the maze, connected to a tracking and analyse system[1]. Mice[1] Mice (n=8 in each group) are intraperitoneally administered with either vehicle, ONO-8590580 (10 mg/kg), or FG-7142 (10 mg/kg). After 30 min, the mice are infused with 15 mg/mL PTZ solution (infusion rate 0.2 mL/min), and the time taken to reveal clonic seizures is measured, and from this the dose administrated is calculated[1]. |
| References: | [1]. Kawaharada S, et al. ONO-8590580, a Novel GABAAα5 Negative Allosteric Modulator Enhances Long-Term Potentiation and Improves Cognitive Deficits in Preclinical Models. J Pharmacol Exp Ther. 2018 Jul;366(1):58-65. |
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| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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