HOMEPRODUCTSSERVICESCOMPANYCONTACTFAQResearchDictionaryPharmaMobileSign Up FREE or Login

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

Abstract
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
Topics
  • 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)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research network!


Choose Username:
Email:
Password:
Verify Password: