Abstract:
:Metabolism of orphanin FQ/nociceptin (OFQ/N) was studied in the spinal cord of rats. The heptadecapeptide was efficiently cleaved by a neutral serine endopeptidase, thus releasing the major metabolite, OFQ/N(1-11), further truncated to the final product, OFQ/N(1-6). Biologic activity of this latter fragment was tested in vivo, after intracerebroventricular and intrathecal injections. Hexapeptide exhibited a bi-phasic effect, causing antinociception up to 10 min after injection, followed by a hyperalgesia. The analgesic effect was blocked by naloxone and hyperalgesia was inhibited by NMDA--and NMDA/glycine site antagonists. The results indicate that shorter nociceptin fragments still possess their biologic activity though possibly acting via receptors other than ORL1.
journal_name
Peptidesjournal_title
Peptidesauthors
Suder P,Kotlinska J,Smoluch MT,Sällberg M,Silberring Jdoi
10.1016/s0196-9781(98)00165-xsubject
Has Abstractpub_date
1999-01-01 00:00:00pages
239-47issue
2eissn
0196-9781issn
1873-5169pii
S0196-9781(98)00165-Xjournal_volume
20pub_type
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