FEBS Letters | |
Association of aminopeptidase N and endopeptidase 24.15 inhibitors potentiate behavioral effects mediated by nociceptin/orphanin FQ in mice | |
Noble, Florence1  Roques, Bernard P1  | |
[1] Département de Pharmacochimie Moléculaire et Structurale, INSERM U266-CNRS URA D 1500, Université René Descartes, UFR des Sciences Pharmaceutiques et Biologiques, 4 Avenue de l'Observatoire, 75270 Paris Cedex 06, France | |
关键词: Nociceptin/orphanin FQ; Metabolism; Selective inhibitor; Aminopeptidase N; Endopeptidase-24.15; Motor activity; Open field; | |
DOI : 10.1016/S0014-5793(96)01476-7 | |
学科分类:生物化学/生物物理 | |
来源: John Wiley & Sons Ltd. | |
【 摘 要 】
The behavioral effects induced by central administration in mice of the endogenous ORL1 (opioid receptor-like1) ligand, nociceptin/orphanin FQ, were investigated in the absence or presence of inhibitors of aminopeptidase N (bestatin) and endopeptidase 24.15 (Z-(l,d)PheΨ(PO2CH2)(l,d)Ala–Arg–Phe) recently shown to be involved in the metabolism of the heptadecapeptide in vitro. A severe reduction in motor activity induced by nociceptin/orphanin FQ was measured in two tests (spontaneous motor activity and open field). This pharmacological effect was shown to be potentiated by the association of bestatin and Z-(l,d)PheΨ(PO2CH2)(l,d)Ala–Arg–Phe, confirming in vivo the involvement of these peptidases in nociceptin/orphanin FQ inactivation. In our conditions, these inhibitors were devoid of intrinsic effects, suggesting a low tonic regulation by the heptadecapeptide of the measured behaviour.
【 授权许可】
Unknown
【 预 览 】
Files | Size | Format | View |
---|---|---|---|
RO201912020303850ZK.pdf | 394KB | download |