Reference

Effect of the histamine H2-receptor antagonist (±)-(E)-1-[2-hydroxy-2-(4-hydroxyphenyl)ethyl]-3'-[2-[[[5-methylamino)me thyl-2-furyl]methyl]thio]ethyl]-2''-(methylsulfonyl)guanidine on acute gastric mucosal injury in rats and its free-radical scavenging activities

Effect of the histamine H2-receptor antagonist (±)-(E)-1-[2-hydroxy-2-(4-hydroxyphenyl)ethyl]-3'-[2-[[[5-methylamino)me thyl-2-furyl]methyl]thio]ethyl]-2''-(methylsulfonyl)guanidine on acute gastric mucosal injury in rats and its free-radical scavenging activities. Naito, Yuji; Yoshikawa, Toshikazu; Matsuyama, Kiichi; Yagi, Nobuaki; Nakamura, Yasunari; Nishimura, Shunichiro; Kaneko, Toshiro; Yoshida, Norimasa; Kondo, Motoharu (First Department Medicine, Kyoto Prefectural Univ. Medicine, Kyoto 602, Japan). Arzneimittel-Forschung, 47(7), 845-848 (English) 1997 Cantor. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The protective effect of T-593 ((±)-(E)-1-[2-hydroxy-2-(4-hydroxyphenyl)ethyl]-3'-[2-[[[5-(methylamino)m ethyl-2-furyl]methyl]thio]ethyl]-2''-(methylsulfonyl)guanidine, CAS 140695-21-2), a new histamine H2-receptor antagonist, was investigated in rats with acute gastric mucosal injury. An ischemic injury followed by reperfusion was produced by applying a small vascular clamp to the celiac artery for 30 min and then removing it for 60 min. T-593 significantly reduced the area of the lesion in the stomach in a dose-dependent manner, and doses of 0.3 and 3.0 mg/kg inhibited the increase of lipid peroxides in the gastric mucosa after ischemia-reperfusion. A spin-trapping method using 5,5-dimethyl-1-pyrroline-N-oxide showed that T-593 scavenged hydroxyl radicals generated by the hydrogen peroxide-ferrous iron sulfate system. T-593 also significantly inhibited the increase of lipid peroxides induced by free-radical initiators in gastric mucosal homogenates. Thus, the protective effect of T-593 against acute gastric mucosal injury induced by ischemia and followed by reperfusion may result, in part, from its antioxidant properties.

Oral antiulcer compositions containing amine derivatives and sucrose fatty acid esters with good bioavailability

Oral antiulcer compositions containing amine derivatives and sucrose fatty acid esters with good bioavailability. Ohashi, Osamu; Arai, Hirotoshi (Toyama Chemical Co., Ltd., Japan). Jpn. Kokai Tokkyo Koho JP 03251527 A2 11 Nov 1991 Heisei, 4 pp. (Japan). CODEN: JKXXAF.There are some reagents with their cas registry numbers 140695-21-2 and 37318-31-3 are used in this study. CLASS: ICM: A61K031-34. ICS: A61K047-26; C07D307-52. APPLICATION: JP 90-46339 27 Feb 1990. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 Oral compns. contain amine derivs. I (R = 4-hydroxyphenyl, 4-carbamoylphenyl, 3-methanesulfonylaminophenyl) or their salts and sucrose fatty acid esters, which show good absorption by oral administration. dl-N-2-Hydroxy-2-(4-hydroxyphenyl)ethyl]-N'-methanesulfonyl-N"-[2-[[5-( methylamino)methyl-2-furyl]methylthio]ethyl]guanidine (II) 15, Ryoto Sugar Ester P 1670 (III; sucrose fatty acid ester) 75, and LH 31 (low substituted hydroxypropyl cellulose) 30 g were mixed, kneaded with 5% EtOH soln. of hydroxypropyl cellulose to give fine granules, which were encapsulated to give capsules. The capsule was orally administered to fasted rats, which showed 6.4% recovery rate of II in urine, vs. 1.3% for a control prepd. similarly but without III. .