Abstract
We successfully discovered peptidomimetic motilin antagonists (17c and 17d) through the improvement of physicochemical properties of a tetrapeptide antagonist (2). Furthermore, with oral administration and based on motilin antagonistic activity, both compounds suppressed motilin-induced colonic and gastric motility in conscious dogs.
MeSH terms
-
Animals
-
Caco-2 Cells
-
Cell Line
-
Drug Discovery
-
Gastrointestinal Agents / antagonists & inhibitors*
-
Gastrointestinal Agents / metabolism
-
Humans
-
Motilin / antagonists & inhibitors*
-
Motilin / metabolism
-
Oligopeptides / chemical synthesis*
-
Oligopeptides / chemistry
-
Oligopeptides / pharmacology
-
Peptides / chemical synthesis
-
Peptides / chemistry*
-
Permeability
-
Rabbits
-
Rats
Substances
-
Gastrointestinal Agents
-
Oligopeptides
-
Peptides
-
Motilin