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Motilin is a 22-amino acid polypeptide hormone secreted primarily by endocrine Mo cells in the duodenum and jejunum. It is released cyclically during fasting and stimulates phase III contractions of the migrating motor complex (MMC), regulating GI motility and preparing the gut for feeding. Motilin also induces secretion of pepsin, pancreatic enzymes, and gastric acid, and influences gallbladder and lower esophageal sphincter contractions. The primary receptor for motilin is the motilin receptor (MLN-R or GPR38), a G protein-coupled receptor located on smooth muscle cells and enteric neurons in the gastrointestinal tract. Motilin and its receptor have been investigated as therapeutic targets for disorders of gastrointestinal motility, but "motilin secretion" itself is not a molecular target; rather, it is the biological process of hormone release.
Drugs act as agonists at the motilin receptor (a GPCR), stimulating GI motility by mimicking motilin effects
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