Disease relevance of EM-523

• These results indicate that EM-523 mimics motilin in stimulating gastrointestinal motility and that this agent may be useful treat gastrointestinal disorders such as gastric stasis, gastroesophageal reflux, and postoperative ileus, and so forth [1].

Psychiatry related information on EM-523

• We investigated the effect of an erythromycin derivative, EM523L, on interdigestive gastrointestinal motor activity and plasma motilin concentrations in three healthy volunteers using an infused catheter system [2].

High impact information on EM-523

• CONCLUSIONS: EM-523-induced phase III-like contractions are brought about through the cholinergic neural pathway and 5-HT3 receptors, and endogenous motilin release is partially involved [3].
• ABT-229 was > 300,000 times more potent than erythromycin in vitro and had 39% oral bioavailability in dog compared to its 4",12-dihydroxy congener (EM-523), which was only 400 times more potent than erythromycin and had relatively low (1.4%) oral bioavailability [4].
• These findings indicate that the contractile activity of EM-523 is very similar to that of motilin and that EM-523 and motilin may share the same site of action [5].
• Cisapride and metoclopramide increased gastrointestinal motility both in the fasting and digestive states; however, their contractile pattern was different from that of EM-523 [1].
• In the fasting state, EM-523 given i.v. or i.d. at 3 micrograms/kg or more induced contractions in the stomach that migrated along the small intestine [1].

Chemical compound and disease context of EM-523

• Effect of intravenous administration of EM523L on gastric emptying and plasma glucose levels after a meal in patients with diabetic gastroparesis: a pilot study [6].

Biological context of EM-523

• A dose of 2 mg EM523L was administered IV over 15 min just after ingestion of a solid meal (200 kcal Gastric emptying was measured by a radionuclide technique [7].

Anatomical context of EM-523

• The rabbit duodenum and jejunum were more sensitive than the ileum to EM-523 and motilin, but no selectivity was observed with PGF2 alpha [5].
• We have studied the ability of the derivative EM-523 [de(N-methyl)-N-ethyl-8,9-anhydroerythromycin A 6,9-hemiacetal] to induce contractions in duodenal smooth muscle strips and to displace labeled motilin bound to antral smooth muscle, in man and in rabbit [8].
• Effect of erythromycin derivative EM523L on human interdigestive gastrointestinal tract [2].

Gene context of EM-523

• We conclude that EM-523 is a potent motilin agonist [8].
• A Schild plot revealed that EM-523 was a competitive inhibitor of motilin receptor binding in man and in rabbit [8].
• EM-523 and motilin induced contractions in the rabbit intestinal preparations but not in the rat or guinea pig preparations [5].
• EM523L, a nonpeptide motilin agonist, stimulates gastric emptying and pancreatic polypeptide secretion [7].

Analytical, diagnostic and therapeutic context of EM-523

• The contractile response to EM-523 or motilin was reduced markedly after treatment of the preparation with a high concentration of either agent, and cross-tachyphylaxis between EM-523 and motilin was also observed [5].
• A total of 2 mg of EM523L dissolved in 100 mL of physiologic saline was administered by intravenous infusion over a period of 15 minutes after ingestion of the test meal [6].

References