Nociceptin induced inhibition of K+ evoked glutamate release from rat cerebrocortical slices

• Published in: British journal of pharmacology 1996-11, Vol.119 (6), p.1081-1083
• Main Authors: Nicol, Beverley, Lambert, David G., Rowbotham, David J., Smart, Darren, McKnight, Alexander T.
• Format: Article
• Language: English
• Subjects: Amino Acid Sequence; Animals; Biological and medical sciences; Central nervous system; Central neurotransmission. Neuromudulation. Pathways and receptors; Cerebral Cortex - drug effects; Cerebral Cortex - metabolism; Dose-Response Relationship, Drug; Female; Fundamental and applied biological sciences. Psychology; glutamate release; Glutamic Acid - metabolism; In Vitro Techniques; Molecular Sequence Data; Naloxone - pharmacology; Nociceptin; Opioid Peptides - pharmacology; orphan receptor; orphanin FQ; Potassium - pharmacology; rat cerebrocortical slices; Rats; Rats, Wistar; Receptors, Opioid - agonists; Vertebrates: nervous system and sense organs
• ISSN: 0007-1188; 1476-5381
• DOI: 10.1111/j.1476-5381.1996.tb16007.x

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 μm)‐insensitive excluding an activation of μ, δ and κ opioid receptors. These data demonstrate the functional coupling of ORL1 in glutamatergic neurones and implicates a role for nociceptin in glutamatergic neurotransmission.