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Literature summary for 4.6.1.1 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
Search for more literature for 4.6.1.1

Activating Compound

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

Cloned(Commentary)

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

Inhibitors

Inhibitors Comment Organism Structure
buprenorphine a low-efficacy partial mu-opioid agonist Homo sapiens
DAMGO a higher efficacy mu-opioid agonist Homo sapiens
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
morphine a higher efficacy mu-opioid agonist Homo sapiens
nalbuphine a low-efficacy partial mu-opioid agonist Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
glioma cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
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