CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).
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.
Sugg
E E
EE
Department of Medicinal Chemistry, Glaxo Research Institute, Research Triangle Park, North Carolina 27709.
Kimery
M J
MJ
Ding
J M
JM
Kenakin
D C
DC
Miller
L J
LJ
Queen
K L
KL
Rimele
T J
TJ
D000595:Amino Acid Sequence; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D005704:Gallbladder / Q000187:drug effects; D006168:Guinea Pigs; D006801:Humans; D066298:In Vitro Techniques; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000494:pharmacology*; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013758:Tetragastrin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D009842:Oligopeptides; D043886:Receptor, Cholecystokinin A; D011949:Receptors, Cholecystokinin; D013758:Tetragastrin; C066278:A 71623