Rebamipide CAS NO.90098-04-7

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1. Introduction of Rebamipide

Rebamipide, with the cas register number of 90098-04-7, can be called (+-)-2-(4-Chlorobenzoylamino)-3-(2(1H)-quinolinon-4-yl)propionic acid, mucosta, proamipide. Rebamipide is a gastroprotective drug, it is a compound selected from over 500 amino acid analogs of 2(1H)-quinolinone tested for gastroprotective action and for efficacy to heal experimental gastric ulcers. This drug stimulates prostaglandin generation in gastric mucosa and improves not only the speed but also the quality of ulcer healing. In addition, it protects the gastric mucosa against acute injury caused by various noxious and ulcerogenic factors.

Specification

2. Basic Information of Rebamipide

Rebamipide, an amino acid derivative of 2(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. It has also been used for the treatment of Beh?et's disease. Some studies have shown effectiveness in presbyacusis (age-related hearing loss).

1) Properties
(1)Polar Surface Area: 95.5;
(2)Index of Refraction: 1.634 ;
(3)Molar Refractivity: 95.077 cm³;
(4)Molar Volume: 265.848 cm³;
(5) Polarizability: 37.692 10-24cm³;
(6)Surface Tension: 58.3219985961914 dyne/cm;
(7)Density: 1.395 g/cm³;
(8)Flash Point: 374.104 °C;
(9)Enthalpy of Vaporization: 106.903 kJ/mol;
(10)Boiling Point: 694.97 °C at 760 mmHg.

2) Toxicity

3) Mechanisms of action and efficacy in mucosal protection and ulcer healing
Rebamipide, a gastroprotective drug, is a compound selected from over 500 amino acid analogs of 2(1H)-quinolinone tested for gastroprotective action and for efficacy to heal experimental gastric ulcers. This drug stimulates prostaglandin generation in gastric mucosa and improves not only the speed but also the quality of ulcer healing. In addition, it protects the gastric mucosa against acute injury caused by various noxious and ulcerogenic factors. Based on these experimental results, rebamipide had been subsequently tested in several clinical trials and approved in Japan for therapeutic use in patients with gastric ulcers and patients with acute gastritis. The main purpose of developing this type of drug was to improve the quality of ulcer healing, especially in that antisecretory drugs lack this advantage. In a preliminary clinical study, rebamipide improved the quality of gastric ulcer healing and reduced future ulcer recurrence. A number of basic research studies have been performed to clarify the mechanisms of rebamipide's action. These studies demonstrated unique properties of rebamipide and convincingly showed that it increases gastric mucus glycoprotein components, stimulates migration and proliferation of wounded epithelial cell monolayers, increases expression of epidermal growth factor and its receptor in normal and ulcerated gastric mucosa, and scavenges active oxygen radicals. The drug also attenuates the activity of neutrophils and the production of inflammatory cytokines stimulated by NSAIDs and/or H. pylori. Therefore, rebamipide can contribute to the management of patients who are taking NSAIDs or are infected with H. pylori. The inhibition of immunoinflammatory responses by rebamipide in H. pylori-infected patients may prevent development of gastritis, peptic ulcer disease, its recurrence, and possibly gastric cancer. Moreover, rebamipide may enhance eradication of H. pylori-infection using standard eradication therapy.