CCK-A Receptor Selective Antagonists Derived from the CCK-A Receptor Selective Tetrapeptide Agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623)

Elizabeth E. Sugg, Millard J. Kimery, Jian Mei Ding, Deborah C. Kenakin, Laurence J. Miller, Kennedy L. Queen, Thomas J. Rimele

Research output: Contribution to journalComment/debate

12 Scopus citations

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 Dor 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.

Original languageEnglish (US)
Pages (from-to)207-211
Number of pages5
JournalJournal of Medicinal Chemistry
Volume38
Issue number1
DOIs
StatePublished - Jan 1 1995

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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