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Opioid Receptor Activity and Analgesic Potency of DPDPE Peptide Analogues Containing a Xylene Bridge

Stefanucci, A. and Novellino, E. and Mirzaie, S. and Macedonio, G. and Pieretti, S. and Szűcs, Edina and Erdei, Anna and Zádor, Ferenc and Benyhe, Sándor (2017) Opioid Receptor Activity and Analgesic Potency of DPDPE Peptide Analogues Containing a Xylene Bridge. ACS MEDICINAL CHEMISTRY LETTERS, 8 (4). pp. 449-454. ISSN 1948-5875

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Abstract

d-Pen2,d-Pen5 enkephalin (DPDPE) is one of the most selective synthetic peptide agonists targeting the delta-opioid receptor. Three cyclic analogues of DPDPE containing a xylene bridge in place of disulfide bond have been synthesized and fully characterized as opioid receptors agonists. The in vitro activity was investigated showing a good affinity of 7a-c for mu- and delta-receptors. In vivo biological assays revealed that 7b is the most potent analogue with the ability to maintain high level of analgesia from 15 to 60 min following intracerebroventricular (i.c.v.) administration, whereas DPDPE was slightly active until 45 min. Compound 7b induced long lasting analgesia also after subcutaneous administration, whereas DPDPE was inactive.

Item Type: Article
Subjects: Q Science / természettudomány > QH Natural history / természetrajz > QH301 Biology / biológia > QH3011 Biochemistry / biokémia
SWORD Depositor: MTMT SWORD
Depositing User: MTMT SWORD
Date Deposited: 25 Jan 2018 07:36
Last Modified: 22 Mar 2018 00:15
URI: http://real.mtak.hu/id/eprint/73292

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