• Title/Summary/Keyword: Gastric secretion.

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Synthesis of Histamine $H_2$-receptor antagonists - Synthesis of 5,6-dihydro[2,1-b]thiazole derivatives - (Histamine $H_2$-수용체길항제의 합성 - 5,6-Dihydroimidazo[2,1-b]thiazole 유도체의 합성 -)

  • 박상우;이강노
    • YAKHAK HOEJI
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    • v.35 no.5
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    • pp.368-371
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    • 1991
  • For the development of new antiulcer agents 5, 6-dihydroimidazo[2, 1-b]- thiazoles substituted at the 3-position are sythesized. Thus, the reaction of 3-chloromethyl-5, 6-dihydroimidazo[2, 1-b]thiazole(2) with thiourea and subsequently with 3-chloro-propionitrile gives 3-[3-[5, 6-dihydroimidazo[2, 1-b]thiazolyl]methylthio]propionitrile(4), which by partial alcoholysis with methanol is converted into methyl-3-[3-[5, 6-dihydro-imidazo[2, 1-b]thiazoyl]methylthio]propionimidate(5) . This compound(5) is treated finally with sulfamide or sulfonamides. 3-[3-[5, 6-dihydroimidazo[2, 1-b]thiazoyl]methylthiol-N$^{2}$-sulfamoyl-propionamidine(6) inhibited gastric acid secretion (45%) when administered intraduodenally (100 mg/kg) to pylorus-ligated rats.

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General Pharmacology of DA-7101, a New Antibiotic Composition (새로운 복합항생제 DA-7101의 일반약리작용)

  • 김정훈;오태영;배은주;손문호;김순회;김원배
    • Biomolecules & Therapeutics
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    • v.7 no.3
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    • pp.285-291
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    • 1999
  • DA-7101 is a new combined formulation of cefatrizine:clavulanic acid (2:1) under development as oral abtibiotics. The general pharmacological properties of DA-7101 on central nervous, cardiovascular, gas-trointestinal and other organ systems were studied by oral administration, in vivo and in vitro. DA-7101 had no marked effects all tests studied such as general behavior, hexobarbital-induced sleeping, spontaneous activity, anticonvulsion, body temperature, acetic acid-induced writhing, rotarod performance, heart rate and blood pressure in cats, isolated ileum movement, intestinal transition, gastric juice secretion and urine volume and electrolytes in rats. But exceptionally at the highest dose of 900 mg/kg, DA-7101 increased hexobarbital-induced sleeping time, caused a slight hypotension and decreased the secretion of gastric juice. These results suggest that at the estimated clinical dose DA-7101 would not bring about any serious acute adverse effects clinically.

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Effect of Leonurus sibiricus green juice on gastric sceretion of Rats (익모초(益母草) 녹즙(綠汁)이 흰쥐의 위액분비기능(胃液分泌機能)에 미치는 영향(影響))

  • Sheo, Hwa-Joong;Lee, Myun-Yul
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.15 no.4
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    • pp.47-50
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    • 1986
  • These studies were carried out to investigate effects of Leonurus sibiricus green juice on gastric secretion of rats and acute toxicity in mice ; $LD_50(mg/kg)$ of Leonurus sibiricus extract was 625mg/kg intraperitoneally in mice. The groups administered green juice and water extract of Leonurus sibiricus showed more excellent increasing effect in total acidity and peptic activity, and decreasing effect on gastric volume than control group. But any differences were not found between sample and control group in gastric pH. It is suggested that Leonurus sibiricus can he used as the bitter stomachics to promote the gastric digestion.

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Evaluation for Protective Effect of Rutin, a Natural Flavonoid, against HCl/Ethanol-Induced Gastric Lesions

  • Jeong, Choon-Sik
    • Biomolecules & Therapeutics
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    • v.17 no.2
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    • pp.199-204
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    • 2009
  • In this study we investigated the protective effects of rutin, a natural plant flavonoid, on HCl/ethanol-induced gastric lesions in rats. Rutin showed the antioxidant activities, the acid-neutralizing capacities, and the inhibitory effects on the growth of Helicobacter pylori (H. pylori.), which are equivalent to control compounds. In addition, rutin significantly inhibited HCl/ethanol-induced gastric lesions. Antigastritic action of rutin may be associated with the antioxidant activities, acid-neutralizing capacities, anti-H. pylori action, and the stimulation of mucus secretion. From these results, we could suggest that rutin may be useful for the treatment and/or protection of gastritis.

The Antigastritic Effect of Taraxaci Herba (포공영의 항위염 작용)

  • Lee, Eun-Bang;Kim, Jung-Keun;Kim, Ok-Kyung
    • Korean Journal of Pharmacognosy
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    • v.24 no.4
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    • pp.313-318
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    • 1993
  • The methanol extract of Taraxaci Herba was found to have inhibitory effect on the gastric lesion induced by HCl-ethanol. The systematic fractionation of the methanol extract resulted in positive action with water fraction in the gastric lesion. It also showed significant inhibition of gastric lesion induced by HCl-aspirin and absolute ethanol, but did not prevent indomethacin induced gastric lesion. This fraction did not affect basal gastric acid secretion but showed a decrease of pepsin activity in pylorus-ligated rats.

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Studies on the Efficacy of Ganoderma lucidum in Digestive System (영지(靈芝)버섯(Ganoderma lucidum)의 소화기계(消化器系)에 대한 약효연구(藥硏究))

  • Chung, Myung-Hyun;Um, Kie-Jin;Lee, Byung-Joo;Rim, Gi-Ryong
    • Korean Journal of Pharmacognosy
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    • v.24 no.2
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    • pp.140-152
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    • 1993
  • This study was attempted to investigate the effect of Ganoderma lucidum extract on digestive system in experimental animals. Ganoderma lucidum water extract (GWE) was found to be promoted the charcol transport rate in the small intestine of mice. GWE exhibited the augmentation of spontaneus movement(motility) and contractile response(tension) in the ileum and colon strips of rabbit, and these action were inhibited by atropine. GWE given intraduodenaly(i.d.) exhibited the significant increase of gastric acid secretion in pylorus-ligated rats. GWE inhibited the formation of some experimental gastric ulcers(pylorus ligation ulcer i.d., indomethacin-induced ulcer p.o., i.d. and aspirin-induced ulcer p.o.) in rats, which are considered to relate to a protective action. GWE and EtOH extract(water soluble phase) were remarkably increase of bile excretion, when administration of i.d., intravenation(i.v.) and per os (p.o.) compared with normal-control group. GWE was observed antibacterial activity aginst several intestinal microoganisms and others bacteria in vitro test.

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Studies on theEfficacy of Machili Cortex in the Digestive System (한국후박(韓國厚朴)(Machili Cortex)의 소화기계(消化器系)에 대한 약효연구(藥效硏究))

  • Lee, Byoung-Joo;Chung, Myung-Hyun
    • Korean Journal of Pharmacognosy
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    • v.25 no.3
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    • pp.278-292
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    • 1994
  • This study was attempted to investigate the effect of Machili Cortex extract(Machilus thunbergii Sieb. et Zucc. ) on digestive system in experimental animals. EtOH and MeOH extracts(E.E. and M.E.) were found to inhibit the charcoal transport rate in the small intestine of mice. E.E. exhibited the inhibition of spontaneous movement(motility) and tension in the ileum and colon strips of rabbit, and these actions were inhibited by action of acetylcholine. E.E. and M.E. given intraduodenaly(i.d.) exhibitied the significant decrease of gastric acid secretion in pylorus-ligated rats. E.E. and M.E. inhibited the formation of some experimental gastric ulcers(pylorus ligation-ulcer i.d., indomethacin-induced ulcer p.o. and aspirin-induced ulcer p.o. ) in rats, which are considered to relate to a protective action. E.E. and M.E. caused remarkable increase of bile excretion, compared with normal-control group, when adminstered through i.d., i.v. and p.o. The antibacterial activity against several intestinal microorganisms and other bacteria in vitro test was observed in the administration of E.E. and M.E.

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Effect of Gaewool-Whadam-Jian on Transport Ability of Small Intestine and Secretion of Gastric Juice in the Rat (개울화담전(開鬱化痰煎)이 흰쥐 소장(小腸) 수송능(輸送能)과 위액분비에 미치는 영향)

  • Kim Hee-Chul;Lee Young-Soo
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.19 no.5
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    • pp.1330-1336
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    • 2005
  • This study was carried out to investigate the motor activity and glucose transport and metabolism of Gaewool-Whadam-Jian(GWJ) in rat gastro-intestinal tract. The motor activity of the rat gastro-intestinal tract has been investigated by means of measuring barium sulfate passage degrees. Atropine treatment significantly delayed barium sulfate transit, and GWJ pretreatment increased intestinal motor activity, but not significant. GWJ administration showed no toxicity to kidney and liver. Transport and metabolism of glucose were studied in everted sac of rat small intestine with incubation under several conditions. The transport and metabolism of glucose were greater at jejunum than ileum. So, everted jejunum of rat were used to study the effect of GWJ. When GWJ were treated, the concentration of glucose were higher than untreated group. This result was thought to be influenced by the glucose in GWJ. When 2, 4 dinitrophenol and phlorizin were treated, the transport and metabolism of glucose were decreased, but GWJ treated together, the concentration of glucose in serosal solution increased. Gastric juice secretion and total acidity significantly decreased by administration of GWJ through duodenum region. The mechanism of effect of GWJ was still unidentified, Dut through continuous investigation, the effect of GWJ should be investigated.

Pharmacological Actions of the Combined Preparations, 'Sahyangsohap-won' and 'Woohwangporyong-hwan' (사향소합원 및 우황포룡환의 약효 연구)

  • Lee, Eun-Bang;Han, Yong-Nam
    • Korean Journal of Pharmacognosy
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    • v.17 no.4
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    • pp.292-301
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    • 1986
  • The combined preparations of the traditional Korean prescriptions, Sahyangsohap-won (A1) and Woohwangporyong-hwan (B1) were evaluated on pharmacological actions in rats and mice, in parallel with the preparations of their modified prescriptions (A2 and B2). The acute toxicities of the four preparations were very low of which $LD_{50}$ values were more than 4g/kg, p.o. and no systematic symptoms were found at the doses. All the preparations showed sedative action by prolongation of sleeping time induced with hexobarbital sodium. The action was more potent in the modified preparations than in the original ones. All the preparations had no anticonvulsant action both in chemoshock seizures induced by pentetrazole and strychnine and in electroshock seizure. In rat fundus preparation, A1 and A2 elicited strong contraction at the concentration of $1{\times}10^{-3}\;g/ml$ in bath, whereas B1 and B2 did neither contraction nor relaxation at the same concentration. The four preparations had no inhibitory effect against acetylcholine induced spasm. In rat intestinal preparation, the four preparations exhibited neither contraction nor relaxation. However, A1 and A2 had antagonistic effect against spasm at the concentration of $1{\times}10^{-3}\;g/ml$. Single administration of each preparation at the dose of 0.24g/kg, p.o. stimulated the secretion of pepsin in rat stomach without inciting the secretion of gastric juice. Their stimulating actions were more marked in B1 and B2 than in A1 and A2, and were more promptly exhibited in the modified preparations (A2 and B2). Accelerating action of bile secretion by single administration of each preparation was found at the dose of 0.24g/kg, p.o. in rats. All the preparations except A2 also stimulated the secretion of bile acid.

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Studies on the effects of central nervous system stimulants and depressant on exocrine pancreas (흰쥐의 담취액 분비에 미치는 수종 중추흥분 및 억제물질의 영향)

  • Park, Suh-Kyung
    • The Korean Journal of Pharmacology
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    • v.12 no.1
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    • pp.15-22
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    • 1976
  • The clinical abuse of C.N.S. stimulants during recent years has directed particular attention. Effect of various organs other than C.N.S. was also extensively investigated with those agents. It has been shown that, although there is a wide variation in sensitivity between species, caffeine stimulates gastric secretion in man, cat, guinea pig and dog. Roth and Ivy(1944) reported that caffeine and histamine acted synergistically in stimulating gastric secretion in the cat. Vaille et al(1966) studied that production of pancreatic juice in the rat was enhanced, but bile secretion was not affected by caffeine. In clinical study the effect of chlorpromazine on the external pancreatic secretion in the 24 subjects, the volume fell more than 20% in 7 subjects. (Skajaa et al 1960) It is widely known that C.N.S. stimulants enhanced spontaneous motor activity in the mice, while tranquilizers depressed the activity. Woo (1975) reported that the group of mice treated with chlorpromazine showed markedly inhibited motor activity and in the group of mice treated with amphetamine, there was a significant increase in the motor activity. The purpose of the present experiment was to study the effects of C.N.S. stimulants and depressant on the exocrine pancreas, and on the spontaneous motor activity in the rats. The results obtained are summarized as follows. 1. In animals treated with xanthine derivatives, the volume of pancreatobiliary secretion was markedly increased. 2. Total bilirubin output was elevated markedly in the xanthine derivatives and imipramine treated animals. The bilirubin concentration was increased in xanthine derivatives treated group. 3. The concentration of cholate in the bile was decreased in the chlorpromazine treated group. 4. The activity of lipase in the pancreatobiliary juice was elevated markedly in the xanthine derivatives treated group only. 5. In the all experimental groups, the activity of amylase in pancreatobiliary juice was significantly elevated. 6. In the caffeine treated group, spontaneous motor activity was markedly increased in $30{\sim}60$ minutes, and the amphetamine treated group showed the increased motor activity in first 30 minutes. 7. The group of rats treated with chlorpromazine showed markedly inhibited motor activity after 30 minutes, and the imipramine treated group showed similar result but less inhibition.

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