Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics

Peptidomimetic motilin antagonists ( 17c and 17d) were identified. Both compounds dose-dependently suppressed motilin-induced colonic and gastric motility in conscious dogs. We successfully discovered peptidomimetic motilin antagonists ( 17c and 17d) through the improvement of physicochemical proper...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-07, Vol.19 (13), p.3426-3429
Hauptverfasser:	Taka, Naoki, Matsuoka, Hiroharu, Sato, Tsutomu, Yoshino, Hitoshi, Imaoka, Ikuhiro, Sato, Haruhiko, Kotake, Ken-ichiro, Kumagai, Yoshikazu, Kamei, Kenshi, Ozaki, Ken-ichi, Higashida, Atsuko, Kuroki, Toshio
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Caco-2 Cells Cell Line Digestive system Drug Discovery Gastrointestinal Agents - antagonists & inhibitors Gastrointestinal Agents - metabolism GM-109 Humans Medical sciences Motilin Motilin - antagonists & inhibitors Motilin - metabolism Motilin receptor antagonist Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacology Peptides - chemical synthesis Peptides - chemistry Peptidomimetics Permeability Pharmacology. Drug treatments Rabbits Rats
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