C-Terminal glycine is crucial for hyperalgesic activity of nociceptin/orphanin FQ-(1–6)

A C-terminal analog of the hexapeptide orphanin FQ/nociceptin-(1–6), [Ala 6]-orphanin FQ/nociceptin-(1–6), and a pentapeptide orphanin FQ/nociceptin-(1–5) were tested in vivo for their analgesic/hyperalgesic activity in the hot-plate test with rats. Replacement of the C-terminal glycine by l-alanine...

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Bibliographic Details
Published in:European journal of pharmacology 2001-05, Vol.419 (1), p.33-37
Main Authors: Kotlińska, Jolanta, Suder, Piotr, Sciubisz, Agnieszka, Łęgowska, Anna, Eilmes, Julita, Rolka, Krzysztof, Silberring, Jerzy
Format: Article
Language:English
Subjects:
Amino Acid Sequence
Analgesics
Animals
Biological and medical sciences
Glycine
Hyperalgesia - chemically induced
Male
Medical sciences
Metabolism
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Nociceptin
Opioid Peptides - chemistry
Opioid Peptides - pharmacology
Opioid receptor
Orphanin FQ/nociceptin
Pain
Pain Measurement
Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems
Pharmacology. Drug treatments
Rats
Rats, Wistar
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Summary:A C-terminal analog of the hexapeptide orphanin FQ/nociceptin-(1–6), [Ala 6]-orphanin FQ/nociceptin-(1–6), and a pentapeptide orphanin FQ/nociceptin-(1–5) were tested in vivo for their analgesic/hyperalgesic activity in the hot-plate test with rats. Replacement of the C-terminal glycine by l-alanine (Phe-Gly-Gly-Phe-Thr-Ala) in orphanin FQ/nociceptin-(1–6) abolished the hyperalgesic potency of native orphanin FQ/nociceptin-(1–6) (Phe-Gly-Gly-Phe-Thr-Gly), but analgesic activity was retained and was diminished by naloxone. Removal of the C-terminal amino acid (glycine or alanine) from orphanin FQ/nociceptin-(1–6) caused a significant loss of analgesic activity. It is anticipated that glycine plays a crucial role in the biphasic activity of orphanin FQ/nociceptin-(1–6). This may suggest the existence of a mechanism for terminating the biological action of orphanin FQ/nociceptin.
ISSN:0014-2999
1879-0712
DOI:10.1016/S0014-2999(01)00955-4