Spinal analgesic activity of orphanin FQ/nociceptin and its fragments |
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Authors: | Michael A King Grace C Rossi Albert H Chang LaShone Williams Gavril W Pasternak |
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Institution: | The George Cotzias Laboratory of Neuro-Oncology, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, New York, NY 10021, USA |
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Abstract: | Previous work reveals that orphanin FQ/nociceptin (OFQ/N) administered supraspinally produces an initial hyperalgesic response followed by analgesia. Spinally, OFQ/N elicits a rapidly appearing, naltrexone-reversible, dose-dependent analgesia in the tailflick assay without any indication of hyperalgesia. Two OFQ/N fragments, OFQ/N (1–7) and OFQ/N (1–11), are active, but far weaker. Blockade of sigma receptors with haloperidol enhances the analgesic potency of spinal OFQ/N, OFQ/N (1–7) and OFQ/N (1–11), but not as dramatically as supraspinal OFQ. Antisense probes targeting the second and third coding exons, but not the first exon, of the cloned mouse OFQ/N receptor (KOR-3) partially block OFQ/N analgesia. |
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Keywords: | Orphanin FQ Nociceptin Analgesia Hyperalgesia KOR-3 ORL-1 |
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