| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369082 | Bioorganic & Medicinal Chemistry Letters | 2015 | 7 Pages |
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.
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Related Topics
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Authors
Jayendra Z. Patel, Stephen Ahenkorah, Miia Vaara, Marek Staszewski, Yahaya Adams, Tuomo Laitinen, Dina Navia-Paldanius, Teija Parkkari, Juha R. Savinainen, Krzysztof Walczyński, Jarmo T. Laitinen, Tapio J. Nevalainen,