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ONO-8590580 is a GABAAα5 negative allosteric modulator which enhances long-term potentiation and improves cognitive deficits in preclinical models. 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 clients.
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
| Molecular Weight | 376.43 |
| Formula | C21H21FN6 |
| CAS Number | 1802661-73-9 |
| Purity | >98% |
| Solubility | DMSO: ≥ 55 mg/mL (Need ultrasonic) |
| Storage | at -20°C |
ONO-8590580, a Novel GABAAα5 Negative Allosteric Modulator Enhances Long-Term Potentiation and Improves Cognitive Deficits in Preclinical Models.
Kawaharada S, et al. J Pharmacol Exp Ther. 2018 Jul;366(1):58-65. PMID: 29674331.
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