Failure of ES 52, a highly potent enkephalinase inhibitor, to affect nociceptive transmission by rat dorsal horn convergent neurones |
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| Authors: | Luis Villanueva Samuel Cadden Djamel Chitour Daniel Le Bars |
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| Affiliation: | 1. Graduate Program in Neuroscience, University of California, Riverside, CA 92521, USA;2. Department of Evolution, Ecology, and Organismal Biology, University of California, Riverside, CA 92521, USA;1. Department of Chemistry, School of Advanced Sciences, Vellore Institute of Technology, Vellore, Tamil Nadu, India, 632014;2. Department of Experimental Biology, Palacky University Olomouc, Faculty of Science, Šlechtitelů 27, 78371 Olomouc, Czech Republic;3. Department of Neurology, University Hospital in Olomouc, I. P. Pavlova 6, 77520 Olomouc, Czech Republic;4. Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacký University, Hněvotínská 5, 77515 Olomouc,Czech Republic;5. Department of Biological and Biochemical Sciences, Faculty of Chemical Technology, University of Pardubice, Studentská 573, 53210 Pardubice, Czech Republic;6. Laboratory of Growth Regulators, Faculty of Science, Palacký University Olomouc, and Institute of Experimental Botany of the Czech Academy of Sciences, Šlechtitelů 27, CZ-78371 Olomouc, Czech Republic;7. Department of Chemistry, Rabindranath Tagore University, Hojai, Assam, India, 782435 |
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| Abstract: | ![]()
The effects of ES 52, a highly potent derivative of the enkephalinase (enkephalin-dipeptidylcarboxypeptidase) inhibitor thiorphan, were studied on nociceptive activities of dorsal horn convergent neurones in the anaesthetized rat. Neither the C-fibre component of the responses elicited by supramaximal electrical stimulation of the hindpaw excitatory receptive fields nor diffuse noxious inhibitory controls triggered by immersion of the tail in 46-48 degrees C waterbaths, were affected by ES 52. Thus we conclude that, in our experimental conditions, modulations of the transmission of nociceptive messages at the spinal level are not greatly modified by specifically blocking the degradation of enkephalins. If a major role for enkephalinase (vs aminopeptidase) in the catabolism of enkephalins at the spinal level can be confirmed, then comparison of the present data with our previous results obtained using the opioid antagonist naloxone, might suggest a predominant role for proenkephalin B products (i.e. dynorphins and/or alpha-neo-endorphin) in modulating nociceptive transmission in the spinal cord. |
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| Keywords: | nociception dorsal horn convergent neurones diffuse noxious inhibitory controls (DNIC) endogenous opiates enkephalins |
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