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

doi:10.1021/jm00001a027

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

Gastroenterology and Hepatology

Research output: Contribution to journal › Comment/debate › peer-review

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 language	English (US)
Pages (from-to)	207-211
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	38
Issue number	1
DOIs	https://doi.org/10.1021/jm00001a027
State	Published - Jan 1 1995

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

Access to Document

10.1021/jm00001a027

Cite this

@article{53b0e9b8e0834b088e7fc023db37fae2,

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

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.",

author = "Sugg, {Elizabeth E.} and Kimery, {Millard J.} and Ding, {Jian Mei} and Kenakin, {Deborah C.} and Miller, {Laurence J.} and Queen, {Kennedy L.} and Rimele, {Thomas J.}",

year = "1995",

month = jan,

day = "1",

doi = "10.1021/jm00001a027",

language = "English (US)",

volume = "38",

pages = "207--211",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "1",

}

TY - JOUR

T1 - CCK-A Receptor Selective Antagonists Derived from the CCK-A Receptor Selective Tetrapeptide Agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623)

AU - Sugg, Elizabeth E.

AU - Kimery, Millard J.

AU - Ding, Jian Mei

AU - Kenakin, Deborah C.

AU - Miller, Laurence J.

AU - Queen, Kennedy L.

AU - Rimele, Thomas J.

PY - 1995/1/1

Y1 - 1995/1/1

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=0029018878&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0029018878&partnerID=8YFLogxK

U2 - 10.1021/jm00001a027

DO - 10.1021/jm00001a027

M3 - Comment/debate

C2 - 7837233

AN - SCOPUS:0029018878

SN - 0022-2623

VL - 38

SP - 207

EP - 211

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 1

ER -

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

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this