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Loratadine analogues as MAGL inhibitors. 2015
Jayendra Z Patel, and
Stephen Ahenkorah, and
Miia Vaara, and
Marek Staszewski, and
Yahaya Adams, and
Tuomo Laitinen, and
Dina Navia-Paldanius, and
Teija Parkkari, and
Juha R Savinainen, and
Krzysztof Walczyński, and
Jarmo T Laitinen, and
Tapio J Nevalainen
School of Pharmacy, Faculty of Health Sciences, University of Eastern Finland, PO Box 1627, FIN-70211 Kuopio, Finland. Electronic address: jayendra.patel@uef.fi.
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.
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