μ type opioid receptors in rat periaqueductal gray‐enriched P2 membrane are coupled to G‐protein‐mediated inhibition of adenylyl cyclase

FEBS Letters

Lee, N.M.¹  Fedynyshyn, J.P.¹ 

[1] Department of Pharmacology, University of California, San Francisco, CA 94143-0450 USA

关键词: Opioid receptor;    G-protein;    Adenylyl cyclase;   

DOI  :  10.1016/0014-5793(89)80921-4

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

The periaqueductal gray (PAG) region of the midbrain has been implicated in both stimulation-produced and opioid-induced analgesia. High-affinity μu-selective opioid-binding sites associated with μu type opioid receptors have been detected in rat PAG-enriched P₂, membranes, and these receptors have been shown to be coupled to guanine nucleotidebinding proteins (G-proteins). In the present study the potential G-protein-mediated coupling of μu type opioid receptors to the inhibition of adenylyl cyclase was examined utilizing in vitro adenylyl cyclase assays. In the presence of Na⁺, opioid agonists inhibited adenylyl cyclase in aμu selective, naloxone reversible, dose dependent, and pertussis toxin sensitive manner. Overall the data suggests that μu type opioid receptors in the rat PAG are coupled to G-protein-mediated inhibition of adenylyl cyclase.

【 授权许可】

Unknown