Inhibition of adenylyl cyclase activity by the cholecystokinin analog SNF 9007 in neuroblastoma x glioma NG108-15 hybrid cells.

The effect of the cholecystokininB (CCKB) receptor-selective cholecystokinin octapeptide (CCK-8) analog SNF 9007 on forskolin-stimulated adenylyl cyclase activity in NG108-15 hybrid cells was measured. The activity of SNF 9007 was compared to the delta opioid agonists D-Pen2-D-Pen5-enkephalin (DPDPE, delta 1 receptor-selective) and Tyr-D-Ala-Phe-Glu-Val-Val-Gly-NH2, (D-Ala2-deltorphin II, delta 2-receptor-selective) because SNF 9007 binds with moderate affinity to delta opioid receptors. SNF 9007 inhibited forskolin-stimulated adenylyl cyclase activity with efficacy similar to DPDPE. IC50 determinations showed that D-Ala2-deltorphin II was the most potent, followed by DPDPE, then SNF 9007 (IC50 values = 0.013, 0.21 and 4.8 microM, respectively). CCK-8 had no effect on adenylyl cyclase activity. The delta 1 receptor-selective antagonist 7-benzylidenenaltrexone hydrochloride (BNTX, 10 nM) had no effect on the activity of any of these agonists, but the delta 2 receptor-selective antagonist naltriben methanesulfonate (NTB, 10 nM) increased IC50 values of all the agonists. Combinations of BNTX and NTB (10 nM each) increased the D-Ala2-deltorphin II IC50 value 12-fold, the DPDPE IC50 value 18-fold and the SNF 9007 IC50 value 26-fold. The effect of the combined delta antagonists on SNF 9007 activity was different from the effect on DPDPE or D-Ala2-deltorphin II activity. These data suggest that the interaction of the CCK-8 analog SNF 9007 with opioid receptors in NG108-15 hybrid cells is different from the interaction of opioid peptides with these receptors.
AuthorsS C Roerig, C L Williams, V J Hruby, T F Burks, G C Rosenfeld
JournalRegulatory peptides (Regul Pept) Vol. 61 Issue 1 Pg. 51-6 (Jan 16 1996) ISSN: 0167-0115 [Print] NETHERLANDS
PMID8701027 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Adenylyl Cyclase Inhibitors
  • Analgesics
  • Enkephalins
  • Enzyme Inhibitors
  • Oligopeptides
  • Peptide Fragments
  • Receptors, Opioid, delta
  • deltorphin II, Ala(2)-
  • SNF 9007
  • Enkephalin, D-Penicillamine (2,5)-
  • Cholecystokinin
  • Adenylyl Cyclase Inhibitors
  • Amino Acid Sequence
  • Analgesics (pharmacology)
  • Cholecystokinin (analogs & derivatives, pharmacology)
  • Enkephalin, D-Penicillamine (2,5)-
  • Enkephalins (pharmacology)
  • Enzyme Inhibitors (pharmacology)
  • Glioma
  • Hybrid Cells (drug effects)
  • Molecular Sequence Data
  • Neuroblastoma
  • Oligopeptides (pharmacology)
  • Pain (physiopathology)
  • Peptide Fragments (pharmacology)
  • Receptors, Opioid, delta (agonists)

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