[Effects of 2-benzyloxycarbonylphenyl trans-4-guanidinomethylcyclohexanecarboxylate hydrochloride monohydrate (TKG01) and its clathrate compound with beta-cyclodextrin (TA903) on experimental gastric ulcers and gastric secretion in rats].
Effects of TKG01 on gastric ulcers and gastric secretion in rats were investigated in comparison with those of TA903, which is the equimolar clathrate compound of TKG01 anhydride with beta-cyclodextrin. The doses were adjusted on a molecular weight basis to include the same amount of TKG01 anhydride. Water-immersion stress ulcers were dose-dependently (100, 300 mg/kg) inhibited by TA903 given orally, but only significantly inhibited by TKG01 (300 mg/kg). TA903, given orally, even in low doses (30, 100 mg/kg) potently inhibited HCl-ethanol ulcers, whereas TKG01 did not inhibit these ulcers. Both TA903 and TKG01, given orally (100, 300 mg/kg), showed similar inhibition of indomethacin ulcers. TA903, given intraduodenally (100, 300 mg/kg), dose-dependently inhibited gastric secretion (volume, acid output and pepsin output) in pylorus-ligated rats, but TKG01 only inhibited pepsin output (100, 300 mg/kg). These results showed that TA903 had a broader spectrum of anti-ulcer effects than TKG01 and the mechanism of TA903 could involve both its cytoprotective activity and its anti-secretory effect.
D000818:Animals; D000897:Anti-Ulcer Agents; D003505:Cyclodextrins / Q000494:pharmacology* / Q000627:therapeutic use; D003509:Cyclohexanecarboxylic Acids / Q000494:pharmacology* / Q000627:therapeutic use; D003912:Dextrins / Q000494:pharmacology*; D000431:Ethanol / Q000037:antagonists & inhibitors; D005744:Gastric Acid / Q000378:metabolism; D005753:Gastric Mucosa / Q000378:metabolism*; D006851:Hydrochloric Acid / Q000037:antagonists & inhibitors; D007213:Indomethacin / Q000037:antagonists & inhibitors; D008297:Male; D010434:Pepsin A / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D013213:Starch / Q000494:pharmacology*; D013276:Stomach Ulcer / Q000209:etiology / Q000517:prevention & control*; D013312:Stress, Physiological / Q000150:complications; D047392:beta-Cyclodextrins
D000897:Anti-Ulcer Agents; D003505:Cyclodextrins; D003509:Cyclohexanecarboxylic Acids; D003912:Dextrins; D047392:beta-Cyclodextrins; D000431:Ethanol; D013213:Starch; C043448:2-benzyloxycarbonylphenyl trans-4-guanidinomethylcyclohexanecarboxylate-beta-cyclodextrin; D010434:Pepsin A; D006851:Hydrochloric Acid; D007213:Indomethacin