Metabolic fate of nociceptin/orphanin FQ in the rat spinal cord and biological activity of its released fragment.

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

Peptides

journal_title

Peptides

authors

Suder P,Kotlinska J,Smoluch MT,Sällberg M,Silberring J

doi

10.1016/s0196-9781(98)00165-x

subject

Has Abstract

pub_date

1999-01-01 00:00:00

pages

239-47

issue

2

eissn

0196-9781

issn

1873-5169

pii

S0196-9781(98)00165-X

journal_volume

20

pub_type

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