Motilin

In 1967 J.C. Brown in Vancouver, B.C. (Canada) recognized that the duodenal extract, the source of secretin, cholecystokinin, VIP, etc., also contains a factor which enhances gastric motor activity. The active principle, motilin, was isolated [131] in pure form and the amino acid sequence of the 22-peptide [132] 

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Moss silver Mostat Series Mothproofing Mothproofing agents Motilin... 

Motilin is a 22-amino acid peptide hormone, secreted by the enterochromaffin cells of the small intestine,... 

Monophasic Preparations Monoxide Mood Disorders Mood Elevators Mood-stabilising Drugs Morbus Alzheimer Morphogens Morpholines Motilin... 

E Wiinsch, E Jaeger, S Knof, R Scharf, P Thamm. On the synthesis of motilin, III Determination of the purity and characterization of [13-norleucine]-motilin and [13-leucine]motilin. Hoppe-Seyler s Z Physiol Chem 357, 467, 1976. 

In the GI tract, different hydrodynamic conditions are present, depending on the fasted or the fed state. Contraction patterns are controlled in terms of electromechanical impulses (myoelectric activity) as well as by various hormones (cholecystokinin, secretin, glucagon, motilin, and insulin, for example). In the fasted state, the motility pattern is regulated by the (interdigestive) migrating myoelectric complex [(I)... 

Erythromycin is an antibiotic in the macrolide family (see Chapter 47) that also has promotility effects because it is a motilin agonist. Erythromycin is used (off-label indication) to accelerate gastric emptying in diabetic gastroparesis and postoperative gastroparesis. Tachyphylaxis will occur, so it cannot be used uninterruptedly for long periods. 

Pharmacodynamics What the drug does to the patient. For example, erythromycin stimulates gut motilin receptors and may induce nausea. The patient may stop taking the erythromycin. 

In addition to these receptors, enkephalins may be involved in some parts of this process, while agents which act on gastric serotonin (5-HT4), dopamine, and motilin receptors accelerate gastric emptying and relieve symptoms in gastroparesis. 

Macrolide antibiotics such as erythromycin directly stimulate motilin receptors on gastrointestinal smooth muscle and promote the onset of a migrating motor complex. Intravenous erythromycin (3 mg/kg) is beneficial in some patients with gastroparesis however, tolerance rapidly develops. It may be used in patients with acute upper gastrointestinal hemorrhage to promote gastric emptying of blood before endoscopy. 

Motilin Polypeptide (22 residues) Controls gastrointestinal muscles... 

Motilin 55 (gastric motor activity-stimulating polypeptide), isolated from porcine intestine by Mutt and Brown 123), stimulates gastric motility and pepsin secretion. 

Wiinsch et al.124) synthesized the fragments 9-22 from [Nle13, Glu14]-motilin and [Leu13, Glu14] -motilin. 

Andersson A., and L. Maler (2002) NMR solution structure and dynamics of motilin in isotropic phospholipid bicellar solution. J. Biomol. NMR 24,103-112. 

Wardle KA, Bingham S, Ellis ES et al. (1996) Selective and functional 5-hydroxytryptamine4 receptor antagonism by SB 207266. Br J Pharmacol 118 665-670 Yamamoto O, Matsunaga Y, Shiba Y et al. (1994) Inhibition of motilin-induced phase III contractions by pentagas-trin in Heidenhain pouch dogs. J Pharmacol Exp Ther 271 1471-1476... 

Title Substituted Diamines Derivatives Useful for Motilin Antagonists S.G Johnson et al., US Patent 6,967,199 (November 22, 2005)... 

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