Orphanin FQ has an inhibitory effect on the guinea pig ileum and the mouse vas deferens

Ge Zhang, Thomas F. Murray, David K. Grandy

Research output: Contribution to journalArticle

38 Citations (Scopus)

Abstract

The activity of the recently isolated endogenous opioid-like peptide orphanin FQ (OFQ) was measured in two classical bioassays of opioid action. OFQ potently and concentration-dependently suppressed the electrically stimulated contractions of the guinea pig ileum (GPI) and the mouse vas deferens (MVD)) with EC50 values of 1.82 ± 0.16 and 2.97 ± 0.01 mM, and E(max) values of 56 ± 3% and 96 ± 4%, respectively. This effect of OFQ, in both the GPI and MVD, was insensitive to the opioid receptor antagonist naloxone. OFQ competed with [3H]diprenorphine binding to μ-, δ or κ- opioid receptors stably expressed in Chinese hamster ovary cell lines with IC50 values of 2.1 ± 0.4, 2.2 ± 0.3, 0.75 ± 0.3 μM, respectively. Low affinity for the classical opioid receptors together with the inability of naloxone to antagonize its effect suggest that the inhibitory action of OFQ is mediated via a distinct OFQ receptor in the GPI and MVD. Consequently, the MVD could serve as a valuable bioassay of potential OFQ receptor antagonists.

Original languageEnglish
Pages (from-to)102-106
Number of pages5
JournalBrain Research
Volume772
Issue number1-2
DOIs
StatePublished - Oct 24 1997
Externally publishedYes

Fingerprint

Vas Deferens
Ileum
Guinea Pigs
Opioid Receptors
Naloxone
Biological Assay
Diprenorphine
Opioid Peptides
Narcotic Antagonists
Cricetulus
Opioid Analgesics
Inhibitory Concentration 50
Ovary
nociceptin
Cell Line

All Science Journal Classification (ASJC) codes

  • Neuroscience(all)

Cite this

Orphanin FQ has an inhibitory effect on the guinea pig ileum and the mouse vas deferens. / Zhang, Ge; Murray, Thomas F.; Grandy, David K.

In: Brain Research, Vol. 772, No. 1-2, 24.10.1997, p. 102-106.

Research output: Contribution to journalArticle

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