| Hazard Information | Back Directory | [Uses]
AKU-005 is a FAAH and MAGL dual inhibitor with IC50 values of 63, 389 nM for rat and human FAAH, respectively. AKU-005 has the potential for the research of trigeminal hyperalgesia[1][2]. | [in vivo]
AKU-005 (0.5 mg/kg; i.p.) shows anti-hyperalgesic and anti-inflammatory effects in rats[1]. | Animal Model: | 150-175 g, Male Sprague Dawley rats (NTG 10 mg/kg; i.p.)[1] | | Dosage: | 0.5 mg/kg | | Administration: | I.p.; 3 h after NTG (nitroglycerin) | | Result: | Significantly prevented the NTG-induced increase in face-rubbing behavior, decreased the CGRP mRNA levels in the meninges, medulla, CSC, and TG ipsilateral, prevented an NTG-induced increase in IL-6 and TNF-alpha mRNA levels in all areas, except for TNF-alpha in the medulla. |
| [References]
[1] Greco R, et al. Effects of the Dual FAAH/MAGL Inhibitor AKU-005 on Trigeminal Hyperalgesia in Male Rats. Cells. 2024 May 13;13(10):830. DOI:10.3390/cells13100830
[2] Aaltonen N, et al. Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase. Chem Biol. 2013 Mar 21;20(3):379-90. DOI:10.1016/j.chembiol.2013.01.012 |
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