| Literature DB >> 25752982 |
Jayendra Z Patel1, Stephen Ahenkorah2, Miia Vaara3, Marek Staszewski4, Yahaya Adams2, Tuomo Laitinen2, Dina Navia-Paldanius3, Teija Parkkari2, Juha R Savinainen3, Krzysztof Walczyński4, Jarmo T Laitinen3, Tapio J Nevalainen2.
Abstract
Compound 12a (JZP-361) acted as a potent and reversible inhibitor of human recombinant MAGL (hMAGL, IC50=46 nM), and was found to have almost 150-fold higher selectivity over human recombinant fatty acid amide hydrolase (hFAAH, IC50=7.24 μM) and 35-fold higher selectivity over human α/β-hydrolase-6 (hABHD6, IC50=1.79 μM). Additionally, compound 12a retained H1 antagonistic affinity (pA2=6.81) but did not show cannabinoid receptor activity, when tested at concentrations ⩽ 10 μM. Hence, compound 12a represents a novel dual-acting pharmacological tool possessing both MAGL-inhibitory and antihistaminergic activities.Entities:
Keywords: 2-Arachidonoyl glycerol; Fatty acid amide hydrolase; Loratadine; Monoacylglycerol lipase; α/β hydrolase-6
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Year: 2015 PMID： 25752982 DOI： 10.1016/j.bmcl.2015.02.037
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823