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

Sandra C. Roerig, Cynthia L. Williams, Victor J Hruby, Thomas F. Burks, Gary C. Rosenfeld

Research output: Contribution to journalArticle

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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 δ opioid agonists D-Pen2 - D-Pen5-enkephalin (DPDPE, δ1 receptor-selective) and Tyr - D-Ala - Phe - Glu - Val - Val - Gly - NH2, (D-Ala2-deltorphin II, δ2-receptor-selective) because SNF 9007 binds with moderate affinity to δ 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 μM, respectively). CCK-8 had no effect on adenylyl cyclase activity. The δ1 receptor-selective antagonist 7-benzylidenenaltrexone hydrochloride (BNTX, 10 nM) had no effect on the activity of any of these agonists, but the δ2 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 δ 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.

Original languageEnglish (US)
Pages (from-to)51-56
Number of pages6
JournalRegulatory Peptides
Volume61
Issue number1
DOIs
StatePublished - Jan 16 1996

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Hybrid Cells
Cholecystokinin
D-Penicillamine (2,5)-Enkephalin
Neuroblastoma
Adenylyl Cyclases
Glioma
Inhibitory Concentration 50
Sincalide
Opioid Receptors
Colforsin
Cholecystokinin Receptors
Peptide Receptors
Opioid Peptides
SNF 9007
Opioid Analgesics
Ala(2)-deltorphin II

Keywords

  • Cyclic adenosine monophosphate (cAMP)
  • Delta opioid receptor
  • Opioid
  • Second messenger

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Neuroscience(all)

Cite this

Inhibition of adenylyl cyclase activity by the cholecystokinin analog SNF 9007 in neuroblastoma × glioma NG108-15 hybrid cells. / Roerig, Sandra C.; Williams, Cynthia L.; Hruby, Victor J; Burks, Thomas F.; Rosenfeld, Gary C.

In: Regulatory Peptides, Vol. 61, No. 1, 16.01.1996, p. 51-56.

Research output: Contribution to journalArticle

Roerig, Sandra C. ; Williams, Cynthia L. ; Hruby, Victor J ; Burks, Thomas F. ; Rosenfeld, Gary C. / Inhibition of adenylyl cyclase activity by the cholecystokinin analog SNF 9007 in neuroblastoma × glioma NG108-15 hybrid cells. In: Regulatory Peptides. 1996 ; Vol. 61, No. 1. pp. 51-56.
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AU - Burks, Thomas F.

AU - Rosenfeld, Gary C.

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N2 - 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 δ opioid agonists D-Pen2 - D-Pen5-enkephalin (DPDPE, δ1 receptor-selective) and Tyr - D-Ala - Phe - Glu - Val - Val - Gly - NH2, (D-Ala2-deltorphin II, δ2-receptor-selective) because SNF 9007 binds with moderate affinity to δ 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 μM, respectively). CCK-8 had no effect on adenylyl cyclase activity. The δ1 receptor-selective antagonist 7-benzylidenenaltrexone hydrochloride (BNTX, 10 nM) had no effect on the activity of any of these agonists, but the δ2 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 δ 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.

AB - 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 δ opioid agonists D-Pen2 - D-Pen5-enkephalin (DPDPE, δ1 receptor-selective) and Tyr - D-Ala - Phe - Glu - Val - Val - Gly - NH2, (D-Ala2-deltorphin II, δ2-receptor-selective) because SNF 9007 binds with moderate affinity to δ 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 μM, respectively). CCK-8 had no effect on adenylyl cyclase activity. The δ1 receptor-selective antagonist 7-benzylidenenaltrexone hydrochloride (BNTX, 10 nM) had no effect on the activity of any of these agonists, but the δ2 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 δ 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.

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