[N-methylnorleucine-(28,31)]cholecystokinin-(26-33) (SNF 8702) activity at a cloned rat CCKB receptor

Richard J. Knapp, Ewa Malatynska, Pam Peterson, Teresa Zalewska, Sunan Fang, Victor J. Hruby, Thomas L. Smith, Henry I. Yamamura

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

[N-methyl-Nle 28,31)]cholecystokinin-(26-33) (SNF 8702) is a highly ligand for the CCKB type of receptor present in the vertebrate central nervous system. Radioligand binding data showing that SNF 8702 binding affinity is reduced by the GTP analog guanylyl-imidodiphosphate suggest that SNF 8702 is an agonist but the ability of SNF 8702 to activate CCKB receptors has not been demonstrated. The present study shows that SNF 8702 is a highly potent agonist at rat CCKB receptors expressed on COS-7 cells and that these receptors are coupled to the mobilization of intracellular calcium. The A50 measured for SNF 8702-induced calcium mobilization (66 pM) is over 6-fold less than that of cholecytstokinin octapeptide (420 pM). Data are also presented showing that SNF 8702 has high binding affinity for these receptors with a Kd value (760 pM) consistent with previous measurements using guinea pig brain tissue preparations.

Original languageEnglish (US)
Pages (from-to)133-138
Number of pages6
JournalEuropean Journal of Pharmacology: Molecular Pharmacology
Volume269
Issue number2
DOIs
StatePublished - Oct 14 1994

Keywords

  • CCK receptor
  • COS-7 cell
  • Calcium mobilization
  • Fura-2
  • Polymerase chain reaction
  • Radioligand binding
  • Transient expression
  • [N-methyl-Nle 2,31)]cholecystokinin-(26-33)

ASJC Scopus subject areas

  • Pharmacology

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