Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates

Monti, L. and Stefanucci, A. and Pieretti, S. and Marzoli, F. and Fidanza, L. and Benyhe, Sándor and Zádor, Ferenc and Szűcs, Edina and Ötvös, Ferenc and Erdei, Anna and Samavati, Reza and Dvorácskó, Szabolcs and Tömböly, Csaba (2016) Evaluation of the analgesic effect of 4-anilidopiperidine scaffold containing ureas and carbamates. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31 (6). pp. 1638-1647. ISSN 1475-6366

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Fentanyl is a powerful opiate analgesic typically used for the treatment of severe and chronic pain, but its prescription is strongly limited by the well-documented side-effects. Different approaches have been applied to develop strong analgesic drugs with reduced pharmacologic side-effects. One of the most promising is the design of multitarget drugs. In this paper we report the synthesis, characterization and biological evaluation of twelve new 4-anilidopiperidine (fentanyl analogues). In vivo hot-Plate test, shows a moderate antinociceptive activity for compounds OMDM585 and OMDM586, despite the weak binding affinity on both μ and δ-opioid receptors. A strong inverse agonist activity in the GTP-binding assay was revealed suggesting the involvement of alternative systems in the brain. Fatty acid amide hydrolase inhibition was evaluated, together with binding assays of cannabinoid receptors. We can conclude that compounds OMDM585 and 586 are capable to elicit antinociception due to their multitarget activity on different systems involved in pain modulation. © 2016 Informa UK Limited, trading as Taylor & Francis Group.

Item Type: Article
Uncontrolled Keywords: PAIN; Opioids; MAGL enzyme; fentanyl; FAAH enzyme
Subjects: Q Science / természettudomány > QH Natural history / természetrajz > QH301 Biology / biológia > QH3011 Biochemistry / biokémia
Depositing User: MTMT SWORD
Date Deposited: 06 Feb 2017 11:05
Last Modified: 06 Feb 2017 11:06

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