• The Korean Journal of Pharmacology
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• v.2 no.1 s.2
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• pp.71-82
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• 1966

The inhibitory effect of 5-hydroxytryptamine (5-HT) on the isolated intestinal strips of the tortoise (Amyda japonica), rat, rabbit and guinea pig was investigated. 1) The strips from the middle or lower part of the tortoise intestine responded with relaxation to 5-HT $(10^{-9}{\sim}10^{-5}g/ml)$, and the magnitude of the relaxation was proportional to the dose of 5-HT. The rectal part of the tortoise intestine, in contrast, showed contraction, the magnitude of which also was proportional to the dose of 5-HT. 2) Various blocking agents such as methysergide, morphine, tetracaine, nethalide, bretylium, hexamethonium, mecamylamine and chlorisondamine, showed no selective blocking activity on the relaxant effect of 5-HT on the tortoise intestine. The inhibitory effect of isoproterenol on the tortoise intestine, however, was selectively blocked by nethalide, and the stimulatory effect of 5-HT on the rectal part of the tortoise was blocked by methysergide. 3) In the presence of 5-HT, the stimulatory effect of DMPP on the tortoise intestine was remarkably attenuated, whereas that of acetylcholine and $BaCl_2$ was little affected. In the presence of isoproterenol, the stimulatory effect of acetylcholine and $BaCl_2$ were affected, but that of DMPP was little affected. 4) Large dose of 5-HT($10^{-4}$g/ml) produced inhibitory effect on the strips from the distal part of the isolated colon of the rat, rabbit and guinea pig, when the strips had been exposed to 5-HT($10^{-4}$g/ml), methysergide or phen`oxybenzamine. 5) Bretylium, as well as nethalide, abolished or remarkably reduced, in a few cases of the experiments, the inhibitory effect of the large dose of 5-HT on the distal part of the colon, whereas morphine did not affect it. 6) The ileal strips of the guinea pig also showed relaxation, as in the colonic strips, having been exposed to the large dose of 5-HT or phenoxybenzamine. This effect, however, was not obsered in the case of the rabbit ileum. 7) The property of the action-site of 5-HT in the tortoise intestine seemd to be different from the 5-HT receptors which have been revealed by several investigators. 8) Adrenergic component seemed to be participated in the inhibitory effect of 5-HT on the colon of the rat and rabbit.

• THE JOURNAL OF KOREAN ORIENTAL ONCOLOGY
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• v.4 no.1
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• pp.1-16
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• 1998

In order to investigate the effect of Bujaleejungtang, by means of oral medication to rats and mice, to isolated intestine and stomach, and the effect to pyloric ulcer, indomethacin-induced ulcer, secretion of gastric juice, and to transport ability of intestine content were studied as the action to G-I tract. The effect to normal rats and resperpine-treated rats were studied as the action to thermo-regulation. The results were as follows: 1. Bujaleejungtang showed the inhibitory effect on the smooth muscle contraction induced by acethylcholine chloride and barium chloride in the isolated mice ileum. 2. Bujaleejungtang showed inhibitory effect on the contraction induced by acetylcholine chloride and barium chloride in the rat fundus-strip. 3. Inhibitory effect of Bujaleejungtang on pyloric ulcer, indomethacin-induced gastric ulcer in rats was statistical recognized(p<0.05). 4. No inhibitory effect of Bujaleejungtang on gastric juice secretion in Shay rats was recognized. 5. Inhibitory effect of Bujaleejungtang on gastric free acidity and total acidity in Shay rats was recognized only when Bujaleejungtang was medicated in high thickness(2000mg/kg) (p<0.001). 6. Inhibitory effect of Bujaleejungtang on pepsin output in Shay rats was recognized only when Bujaleejungtang was medicated in high thickness(2000mg/kg)(p<0.001). 7. Inhibitory effect of Bujaleejungtang on barium sulfate transport in the small intestine of mice was recognized only when Bujaleejungtang was medicated in high thickness(2000mg/kg)(p<0.05). 8. Inhibitory effect of Bujaleejungtang on barium sulfate transport in the large intestine of mice was recognized(p<0.05). 9. Inhibitory effect of Bujaleejungtang on rectal temperature in normal rats was recognized. 10. Inhibitory effect of Bujaleejungtang on rectal temperature in reserpine-treated rats was recognized only when Bujaleejungtang was medicated in high thickness(2000mg/kg)(p<0.05).

• YAKHAK HOEJI
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• v.36 no.1
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• pp.17-25
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• 1992

The general and some other pharmacological actions of growth hormone without N-terminal methionine(rhGH) were investigated in animals. The hormone had no influences on the central nervous system and on body temperature at a high oral dose of 40 IU/kg in animals. It had neither analgesic nor antiepileptic actions at the high doses. In the isolated ileum and trachea of guinea-pig and isolated stomach fundus and uterus of rat, it showed neither contractive nor relaxing effects at a concentration of $1{\times}10^{-3}\;IU/ml$ in bath, and no inhibitory action at a dose of $1{\times}10^{-3}\;IU/ml$ against the contractions produced by histamine ($5{\times}10^{-5}\;g/ml$), serotonin($1{\times}10^{-5}\;g/ml$), acetylcholine($1{\times}10^{-5}\;g/ml$) and oxytocin($5{\times}10^{-3}\;IU/ml$). Furthermore, the intravenous injection of 20 IU/kg rhGH had no influences on the normal blood pressure and respiration in rabbits. These negative results in pharmacological profile are thought that the hormone may not elicit serious side effects. On the other hand, the rhGH exhibited a weak inhibitory action of glucose tolerance in normal rats, significantly lowered the blood glucose contents in adrenalectomized rats 20 min after i.v. administration of 80 IU/kg, and showed a significant inhibitory effect on in vitro glycerol release in epinephrine-stimulated epididymal fat pad segments of rats.

• Biomolecules & Therapeutics
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• v.12 no.2
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• pp.114-121
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• 2004

This study was undertaken to evaluate the general pharmacological properties of CJ-11828, an amlodipine adipate, in experimental animals and in vitro system. CJ-11828 had no effects on general behavior, motor coordination, writhing syndromes, pentetrazol-induced chemoshock and electric shock in mice at dose levels of 3,10, anti 30 mg/kg, po. But there were decrease of body temperature, prolongation of sleeping time, and inhibition of intestinal activity in mice treated with CJ-11828 at doses of 10 and 30 mg/kg, po. CJ-11828 decreased the blood pressure in coscuous fog at the dose level of 2mg/kg, po, but it was expected as a result of pharmacological activity of CJ-11828. Any effect on respiratory system was not observed in conscious rat at doses of 3,10, and 30 mg/kg, po. The slight decrease in spontaneous motor activity was observed in mice treated with CJ-11828 at high dose, 30 mg/kg. In vitro experiments, CJ-11828 had no effect on agonists-induced contraction of isolated guinea pig ileum at 0.1, 1, and 10 ${\mu}$M. Based on these results, it was concluded that CJ-11828 had no pharmacological effect ill these studies even up to the 36-fold anticipated clinical dose, 3 mg/kg.

• Toxicological Research
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• v.26 no.3
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• pp.223-232
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• 2010

Artesunate, a semi-synthetic derivative of artemisinin, is used primarily as a treatment for malaria. Its effects on the central nervous system, general behavior, and cardiovascular, respiratory, and other organ systems were studied using mice, rats, guinea pigs, and dogs. Artesunate was administered orally to mice at doses of 125, 250, and 500 mg/kg and to rats and guinea pigs at 100, 200, and 400 mg/kg. In dogs, test drugs were administered orally in gelatin capsules at doses of 50, 100, and 150 mg/kg. Artesunate induced insignificant changes in general pharmacological studies, including general behavior, motor coordination, body temperature, analgesia, convulsion modulation, blood pressure, heart rate (HR), and electrocardiogram (ECG) in dogs in vivo; respiration in guinea pigs; and gut motility or direct effects on isolated guinea pig ileum, contractile responses, and renal function. On the other hand, artesunate decreased the HR and coronary flow rate (CFR) in the rat in vitro; however, the extent of the changes was small and they were not confirmed in in vivo studies in the dog. Artesunate increased hexobarbital-induced sleeping time in a dose-related manner. Artesunate induced dose-related decreases in the volume of gastric secretions and the total acidity of gastric contents, and induced increases in pH at a dose of 400 mg/kg. However, all of these changes were observed at doses much greater than clinical therapeutic doses (2.4 mg/kg in humans, when used as an anti-malarial). Thus, it can be concluded that artesunate is safe at clinical therapeutic doses.

• Biomolecules & Therapeutics
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• v.13 no.1
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• pp.26-31
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• 2005

The present study examined effects of a water-soluble fraction from mulberry leaves (ML water fraction) on the circulatory and autonomic nervous systems, which were compared with those of acetylcholine (ACh) used as a reference drug in order to elucidate its mechanism of action. Intravenous administration of ACh or a ML water fraction produced temporary depressor and tachycardiac responses in a dose-dependent manner in unrestrained, conscious Sprague-Dawley rats. The systemic hemodynamic effects of ACh and a ML water fraction were almost completely blocked by pretreatment with atropine, a muscarinic antagonist. The depressor responses to ACh and a ML water fraction were slightly enhanced and prolonged by pretreatment with neostigmine, an anticholinesterase, whereas the tachycardiac responses were remarkably blocked by pretreatment with pentolinium, a ganglionic blocking agent. In vitro experiments using the ileum isolated from rats showed that ACh and a ML water fraction increased ileal contractility in a dose-dependent manner. The increases in ileal contractility were also completely abolished in the presence of atropine. Finally, the specific binding of [$^3H$]quinuclidinyl benzilate, a muscarinic antagonist, to rat cortical synaptic membranes was inhibited by a ML water fraction in a concentration-dependent manner with an IC$_{50}$ value of 9.5 mg/ml. The results suggest that the effects of a ML water fraction are mediated through direct stimulation of muscarinic cholinergic receptors by unknown cholinomimetic substance(s) contained in that fraction.

• Toxicological Research
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• v.16 no.3
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• pp.211-219
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• 2000

The therapeutic effect of AS2-006A, a derivative of asiaticoside, has been studied and is being developed as a new wound-healing agent. In the present study, the general pharmacological effects on 1) central nervous system, 2) autonomic nervous system, 3) respiratory system, 4) gastrointestinal system. 5) cardiovascular system. and 6) urinary system were assessed in experimental animals and in in vitro models. 1. In vivo animal study: External applications of the 1 % gel ointment of AS2-006A to rats at the doses of 200. 600 or 2000 mg/kg body weight showed no observable pharmacological effects. The effects on the central nervous system were assessed by observation of behavior, hexobarbital-induced sleeping time, pentetrazole-induced convulsion assay, body temperature measurements, and observations on spontaneous activity and catalepsy. The gel ointment exhibited no effects on the cardiovascular system (i.e. blood pressure and heart rate), renal physiology (i.e. urine volume and electrolytes excretion) and gas-trointestinal physiology (i.e. intestinal charcoal propulsion and gastric mucosal irritation). 2. In vitro experiments: The effects of AS2-006A on the physiology of smooth and cardiac muscles were assessed. Muscle contractions were isotonically and isometrically measured in organ chambers using a physiograph. Cumulative additions of AS2-006A (10$^{-9}$ -10$^{-5}$ M) induced no changes in the tension of isolated guinea pig ileum and tracheal muscles. AS2-006A only slightly increased contractility of rat atrial and papillary muscles at 10$^{-2}$ M, which was not statistically different from control. These data showed that the gel ointment of AS2-006A could be externally applied as a wound-healing agent with no potential side effects.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1995.04a
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• pp.106-106
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• 1995

A polysaccharide, G009, isolated from Ganoderma lucidum IY009 subjected to investigating on general pharmacology. This material at the large oral doses of 1000 and 2000mg/kg in mice did neither exhibit any abnormal behaviors nor effects on central nervous system. It also had no influences on hexobarbital-induced sleeping time, rotarod test and spontaneous activity test at each oral dose of 1000mg/kg in mice. No effects on the body temperature and on acetic acid induced writhing syndrome in mice were observed with its oral administration at 1000mg/kg, and the convulsions induced by strychnine and pentetrazole were not inhibited at its oral doses of 1000mg/kg in mice. The solution of G009 as given intravenously at the doses of 30 and 60mg/kg in rabbit had no influences on blood pressure and respiration rates and depth. In isolated organs of rat uterus and fundus muscles and guinea-pig ileum and trachea, it did not show any contraction or relaxation at the concentration of 2$\times$10$^{-3}$g/ml, and the contractive actions produced by oxytocin, acetylcholine, serotonin and histamine did not inhibited by the same doses. This material showed no effect on intestinal propulsion test in mice and gastric secretion in rats at the oral doses of 1000mg/kg. However, it is interesting that the material exhibited potent inhibition of acidified aspirin induced gastric damage at the doses of 500 and 1000mg/kg in rats.

• Biomolecules & Therapeutics
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• v.2 no.4
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• pp.369-375
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• 1994

A polysaccharide, G009, isolated from Ganoderma lucidum IY 009, was subjected to investigating on general pharmacology. This material at the large oral doses of 1000 and 2000 mg/kg in mice did not exhibit any abnormal behaviors and another effects on central nervous system. It also had no influences on hexobarbital-induced sleeping time, rotarod test and spontaneous activity test at each oral dose of 1000 mg/kg in mice. No effects on the body temperature and on acetic acid induced writhing syndrome in mice were observed with its oral administration at 1000 mg/kg, and the convulsions induced by strychnine and pentetrazole were not inhibited at its oral doses of 1000 mg/kg in mice. The solution of G009 as given intravenously at the doses of 30 and 60 mg/kg in rabbit had no influences on blood pressure and respiration rates and depth. In isolated organs of rat uterus and fundus muscles and guineapig ileum and trachea, it did not show any contraction or relaxation at the concentrations of 2$\times$10$^{-3}$ g/ml, and the contractive actions produced by oxytocin, acetylcholine, serotonin and histamine were not inhibited at the same doses. This material showed no effect on intestinal propulsion test in mice and gastric secretion in rats at the oral doses of 1000 mg/kg. However, it is interesting that the material exhibited potent inhibition of acidified aspirin induced gastric damage at the doses of 500 and 1000 mg/kg in rats.

• The Journal of Internal Korean Medicine
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• v.22 no.1
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• pp.29-38
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• 2001

When I evaluated the component variation of Naesowhajung-tang by the three types of extraction method, and each type's effects on the gastrointestinal tract, I got the following results. 1. The output ratio of extracts made out of Naesowhajung-tang were not significantly different among 13.8% of water extract(Sample-I), 13.5% of 50% ethanol extract(Sample-II), and 15.6% of water extract by spray dryer(Sample-III). 2. magnolol, honokiol, hesperidin, naringin, poncirin and glycyrrhizin Sample II had the largest amount of the following contents: magnolol, honokiol, hesperidin, naringin, poncirin and glycyrrhizin. 3. All the extracts of Naesowhajung-tang showed the inhibitory effect on the smooth muscle contraction of the isolated ileum in mice and fundus-strip in rats induced by acetylcholine chloride and barium chloride. 4. High concentration Sample-II was recognized to be effective in preventing gastric ulcers in Shay's rats. but not in the other rat group. 5. All the extracts of Naesowhajung-tang were recognized to be effective in preventing gastric ulcers induced by Ethanol-HCl in rats. 6. The increase of transport ability in the small intestine was recognized only when the concentration of all the samples was doubled, but not in the other concentrations. 7. The increase of transport ability in the large intestine was recognized only when the concentration of Sample-II was doubled, but not in other concentration. Using the results mentioned above, I suggest that Sample-II has more significant effects on the gastrointestinal tract than the others.