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Literature summary extracted from

  • Clark, M.J.; Linderman, J.J.; Traynor, J.R.
    Endogenous regulators of G protein signaling differentially modulate full and partial mu-opioid agonists at adenylyl cyclase as predicted by a collision coupling model (2008), Mol. Pharmacol., 73, 1538-1548.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
4.6.1.1 forskolin leads to cAMP accumulation in C6 glioma cells expressing the mu-opioid-receptor Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
4.6.1.1 expressed in C6 glioma cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
4.6.1.1 buprenorphine a low-efficacy partial mu-opioid agonist Homo sapiens
4.6.1.1 DAMGO a higher efficacy mu-opioid agonist Homo sapiens
4.6.1.1 additional information maximal inhibition of forskolin-stimulated adenylyl cyclase by buprenorphine and nalbuphine is increased in cells expressing regulator of G protein signaling RGS-insensitive Galphao CIGS, Galphai2 CIGS, or Galphai3 CIGS compared with their GalphaCI counterparts, but the RGS-insensitive mutation has little or no effect on the maximal inhibition by DAMGO and morphine Homo sapiens
4.6.1.1 morphine a higher efficacy mu-opioid agonist Homo sapiens
4.6.1.1 nalbuphine a low-efficacy partial mu-opioid agonist Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
4.6.1.1 ATP Homo sapiens
-
 3',5'-cyclic-AMP + diphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
4.6.1.1 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
4.6.1.1 glioma cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4.6.1.1 ATP
-
 Homo sapiens 3',5'-cyclic-AMP + diphosphate
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
4.6.1.1 additional information
-
 additional information inhibition of forskolin-stimulated adenylyl cyclase by mu-opioid recptor agonists in cells expressing different forms of G proteins, overview Homo sapiens