title: Nociceptin induced inhibition of K+ evoked glutamate release from rat cerebrocortical slices.
abstract: Nociceptin, an endogenous ligand for the orphan receptor ORL1, has recently been described. In this study we have shown that nociception inhibits 46 mM K(+)-stimulated glutamate release from rat perfused cerebrocortical slices with an IC50 of 51 nM. At 100 nM the inhibition amounted to 68 +/- 14% and was naloxone (10 microM)-insensitive excluding an activation of mu, delta and kappa opioid receptors. These data demonstrate the functional coupling of ORL1 in glutamatergic neurones and implicates a role for nociceptin in glutamatergic neurotransmission.
authors.affiliation: University Department of Anaesthesia, Leicester Royal Infirmary.
authors.forename: B
authors.initials: B
authors.lastname: Nicol
authors.forename: D G
authors.initials: DG
authors.lastname: Lambert
authors.forename: D J
authors.initials: DJ
authors.lastname: Rowbotham
authors.forename: D
authors.initials: D
authors.lastname: Smart
authors.forename: A T
authors.initials: AT
authors.lastname: McKnight
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects* / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D005260:Female; D018698:Glutamic Acid / Q000378:metabolism*; D066298:In Vitro Techniques; D008969:Molecular Sequence Data; D009270:Naloxone / Q000494:pharmacology; D018847:Opioid Peptides / Q000494:pharmacology*; D011188:Potassium / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D011957:Receptors, Opioid / Q000819:agonists*; D000097629:Nociceptin
chemical_list: D018698:Glutamic Acid; D009270:Naloxone; D018847:Opioid Peptides; D011188:Potassium; D011957:Receptors, Opioid; D000097629:Nociceptin