Potent and selective, competitive motilin receptor antagonist (IC50
= 4.9 nM). Selective for the motilin receptor over a range of other receptors and ion channels. Inhibits motilin-induced duodenal muscle contractions in vitro
. Also inhibits motilin-induced colonic and abdominal contractions in vivo
. Orally active.
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Oral administration of MA-2029, a novel selective and competitive motilin receptor antagonist, inhibits motilin-induced intestinal contractions and visceral pain in rabbits.
Sudo et al.