CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623)

J Med Chem. 1995 Jan 6;38(1):207-11. doi: 10.1021/jm00001a027.

Abstract

Analogs of the CCK-A receptor selective agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623) were prepared in which the lysine residue was replaced with L-4-aminophenylalanine and D-or L-3-aminophenylalanine. These new analogs were moderately potent antagonists of CCK-8 in the isolated guinea pig gallbladder with exceptional CCK-A receptor selectivity as evaluated in membrane preparations from CHO K1 cells stably transfected with human CCK-A and CCK-B receptors.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • CHO Cells
  • Cricetinae
  • Gallbladder / drug effects
  • Guinea Pigs
  • Humans
  • In Vitro Techniques
  • Molecular Sequence Data
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / pharmacology*
  • Receptor, Cholecystokinin A
  • Receptors, Cholecystokinin / antagonists & inhibitors*
  • Receptors, Cholecystokinin / metabolism
  • Tetragastrin / analogs & derivatives*
  • Tetragastrin / chemical synthesis
  • Tetragastrin / pharmacology

Substances

  • Oligopeptides
  • Receptor, Cholecystokinin A
  • Receptors, Cholecystokinin
  • Tetragastrin
  • A 71623