• Biomolecules & Therapeutics
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• v.2 no.2
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• pp.173-184
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• 1994

The general and some pharmacological actions of DWP 305 were investigated in animals and the following results were obtained. In central nervous system, DWP 305 had no effects on the pentobarbital induced anaesthesia, locomotor activity, rotarod test, traction test, analgesic action in mice and body temperature in rat. DWP 305 showed no depressive action on convulsion induced by strychnine, electronic shock and pentylenetetrazole. From these results, DWP 305 was considered to have no pharmacological effect on the central nervous system. Furthermore, DWP 305 had no influences on the normal blood pressure and heart rate. In the isolated ileum of guinea pig, DWP 305 inhibited contractive effects against the acetylcholine (10$^{-6}$ g/mι), histamine (10$^{-6}$ g/mι), 5-hydroxytryptamine (10$^{-6}$ g/mι) and BaCl$_2$(10$^{-4}$ g/mι) at a concentration of 2.15$\times$10$^{-4}$ g/ml in bath. In the isolated trachea and vats deference, DWP 305 showed no effect on the contractions produced by histamine and norepinephrine, respectively. DWP 305 showed inhibitory effect on the contractions produced by acetylcholine and oxytocin at a concentration of 2.15$\times$10$^{-4}$ g/ml on the isolated nonpregnant rat uterus. DWP 305 had no effect on the isolated right atrium of guinea pig, bile excretion, urine volume, pH, gastrointestinal motility, gastric secretion and blood aggregation.

• The Korean Journal of Physiology and Pharmacology
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• v.4 no.1
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• pp.33-40
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• 2000

This study was designed to clarify the mechanism of the inhibitory action of a nitric oxide (NO) donor, 3-morpholino-sydnonimine (SIN-1), on contraction, cytosolic $Ca^{2+}$ level $([Ca^{2+}]_i)$ and ionic currents in guinea-pig ileum. SIN-1 $(0.01{\sim}100\;{\mu}M)$ inhibited 25 mM KCl- or histamine $(10\;{\mu}M)-induced$ contraction in a concentration-dependent manner. SIN-1 reduced both the 25 mM KCl- and the histamine-stimulated increases in muscle tension in parallel with decreased $[Ca^{2+}]_i.$ Using the patch clamp technique with a holding potential of -60 mV, SIN-1 $(10\;{\mu}M)$ decreased peak Ba currents $(I_{Ba})$ by $30.9{\pm}5.4%$ (n=6) when voltage was stepped from -60 mV to +10 mV and this effect was blocked by ODQ $(1\;{\mu}M),$ a soluble guanylyl cyclase inhibitor. Cu/Zn SOD (100 U/ml), the free radical scavenger, had little effect on basal $I_{Ba},$ and SIN-1 $(10\;{\mu}M)$ inhibited peak $I_{Ba}$ by $32.4{\pm}5.8%$ (n=5) in the presence of Cu/Zn SOD. In a cell clamped at a holding-potential of -40 mV, application of $10\;{\mu}M$ histamine induced an inward current. The histamine-induced inward current was markedly and reversibly inhibited by $10\;{\mu}M$ SIN-1, and this effect was abolished by ODQ $(1\;{\mu}M).$ In addition, SIN-1 markedly increased the depolarization-activated outward $K^+$ currents in the all potential ranges. We concluded that SIN-1 inhibits smooth muscle contraction mainly by decreasing $[Ca^{2+}]_i$ resulted from the inhibition of L-type $Ca^{2+}$ channels and the inhibition of nonselective cation currents and/or by the activation of $K^+$ currents via a cGMP-dependent pathway.

• Korean Journal of Pharmacognosy
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• v.21 no.2
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• pp.163-172
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• 1990

These studies were conducted to investigate the effects of Tongkwan-San water extract on analgesic, sedatative, anti-inflammatory, blood pressure and vasodilating actions, the relaxing action of isolated ileums and actions on the contact dermatitis induced by picryl chloride and on the leakage of the dye into the peritoneal cavity. The results of these studies were summarized as follows: The analgesic effect of Tongkwan-San was noted. The prolongation of anesthetic time of Tongkwan-San was recognized. Spontaneous motilities of isolated ileum of mice were strongly suppressed by Tongkwan-San. It inhibited the contractions of isolated ileum of mice induced by acetylcholine and barium chloride and the contraction of isolated ileum of guinea-pig induced by histamine. Inhibition of the contact dermatitis induced by picryl chloride was recognized. Anti-inflammatory effects in the paw edema induced by histamine and dextran were significantly shown. The leakage of dye into the peritoneal cavity in mice was significantly inhibited. Hypotensive and vasodilating action due to vascular smooth muscle relaxation were noted in rats and rabbits.

• Journal of Pharmaceutical Investigation
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• v.16 no.1
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• pp.18-23
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• 1986

Anemarrhenae Rhizoma has been clinically used as a sedative drug in oriental medicine. We observed the sedative action and effect on the movement of isolated-ileum with each water extract of Anemarrhenae Rhizoma (F-I), saline solution treated preparation (F-II) and 25% ethanol treated preparation (F-III). The results obtained were summerized as follows; 1) Sedative actions were recognized with F-I, F-II and F-III. 2) Prolonged effect of sleeping time was recognized significantly with F-I, F-II and F-III. 3) Each fraction of Anemarrhenae Rhizoma showed the released action on the isolated-ileum of the mouse, rat, rabbit and guinea pig, and antagonic action against contraction induced by acetylcholine, barium chloride and histamine. Thus the mechanism in the released action of the smooth muscle was partly considered as the direct dependence of the smooth muscle.

• Korean Journal of Pharmacognosy
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• v.20 no.3
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• pp.188-195
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• 1989

Hyangsayangwee-Tang, a combined preparation of crude drugs, which has been used for stomach and intestinal disorder, was examined for anti-spasmodic, anti-ulcerative and anti-emetive effects. Spontaneous motility of isolated ileum was strongly suppressed and inhibitory effects against contraction of isolated ileum induced by acetylcholine and barium chloride were shown in mice. And, contraction of isolated guinea-pig ileum by histamine was inhibited. In rats fundus preparations, Hyangsayangwee-Tang elicited strong relaxation and had antagonist effects against the spasm induced by acetylcholine and barium chloride. A significant inhibitory effect on the intestinal propulsion of barium sulfate in mice was shown. In pylorus-ligated rats, Hyangsangwee-Tang inhibited gastric secretion and showed a strong anti-peptic activity. Protective effects against gastric ulceration induced by pyloric ligation, water-immersion stress, histamine and aspirin were significantly recognized in mice and rats. Hyangsayangwee-Tang decreased cupric sulfate-induced vomitting in frogs.

• The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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• v.13 no.1
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• pp.1-21
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• 2000

This experiment was performed to study of Gagambipachungpe-Eum extract solution's effects on acne. Anti-inflammatory edema, anti-histamine, vascular permeability, acne by induced oleic acid, ileum contraction of mice and guinea-pig was measured by oral administration, topical application or both of the sample to the acne of the experimental animals. Dose of samples were taken by 500 and 1,500mg/dl at the experiments. The results were as follows. 1. Gagambipachungpe-Eum on rat hind paw edema induced by $0.5\%$ Carrageenin have statistically significant effects on anti-inflammatory edema at 2, 3(p<0.05) and 4 hours(p<0.01) of the high density 1500mg/kg - oral administration group as compared with sample group. 2. Gagambipachungpe-Eum on rat hind paw edema induced by $1.0\%$ Dextran have statistically significant effects on anti-inflammatory edema at 2 and 4 hours of the high density 1,500mg/kg oral administration group as compared with sample group(p<0.05). 3. Gagambipachungpe-Eum on mouse hind paw edema induced by $1.2\%$% Histamine have statistically significant effects on anti-inflammatory edema at 30, 60 and 90 minutes of the high density 1500mg/kg - oral administration group as compared with sample group(p<0.05). 4. Only high density 1,500mg/kg - oral administration group of Gagambipachungpe-Eum as compared with sample group have significant effects on increased vascular permeability induced by histamine, picryl chloride induced contact dermatitis(p<0.01) and writhing syndrome induced by $0.7\%$ acetic acid(p<0.05) in mice. 5. All of the sample groups, Sample-Ⅰ(orally administered), Sample-Ⅱ(topically administered 500mg/kg), Sample-Ⅲ(topically administered 1,500mg/kg), Sample-Ⅳ(administered simultaneous orally and topically) on acne induced by o1eic acid in rabbit ears has the significant recovery on induced acne after 14 days 6. Gagambipachungpe-Eum have the effects on the motility of the isolated mice ileum, on the contraction induced by acetylcholine chloride and barium chloride in the isolated mice ileum and on the contraction induced by acetylcholine chloride, barium chloride and histamine in the isolated Guinea-pig ileum. According to the about results, it is expected Gagambipachungpe-Eum could be applicable to the treatment of acne.

• Biomolecules & Therapeutics
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• v.9 no.3
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• pp.224-230
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• 2001

DKY is an oriental drug preparation composed of 17 natural products and is known to have antihyperglycemic action at 100 mg/kg po in animal tests. The general pharmacological properties of DKY preparation were investigate in mice, rats, guinea pigs and rabbits. This preparation did neither show any effects on central nervous system, nor effects on algesia, nor epilepsia at the large doses of 3000 mg/kg po in mice or rats. However, the preparation showed hypothermic action at the doses of 330 and 1000 mg/kg po. In the guinea pig ileum, rat fundus strip and estrogenized rat uterus, DKY did not influence their tension at a concentration of 3$\times$10$^{-3}$ g/ml, and the spasmogenic actions produced by histamine, ACh and 5-HT were not blocked in the presence of DKY at 3$\times$10$^{-3}$ g/ml. The blood pressure and respiration were not considerably influenced at 10 mg/kg iv of DKY in rabbits. It did not influence the intestinal propulsion of mice and the normal gastric secretion of rats. These results may suggest that DKY preparation have little effects on central nervous, autonomic and gastrointestimal systems, except hypothermic action.

• Biomolecules & Therapeutics
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• v.5 no.4
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• pp.412-418
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• 1997

General pharmacological properties of AG 60 (mixture of acriflavine and guanosine (1:1, w/w)), which has anticancer effect, following intramuscular administration were examined in terms of effects on central nervous system, gastrointestinal system, cardiovascular system, respiratory system and autonomic nervous system in mice, rats, guinea-pigs and rabbits. AG 60 at the dose of 15 mgtg had no influences on pentobarbital sleeping time, spontaneous motor activity, chemoshock produced by pentylenetetrazole solution, writhing syndromes induced by 0.8% acetic acid solution, and motor coordination of mice. However, AG 60 at the dose of 7.5 and 15 mg/kg caused significant decrease of normal body temperature 1 and/or 2 h after the administration. No influence on body temperature was observed at 3.75 mg/kg in mice. Gastric secretion of rat and intestinal motility of mice were not influenced by the dose of 15 mg/kg. In terms of autonomic nervous system, AG 60 did not show direct effect and inhibitory or augmentative action of histamine- or acetylcholine-induced contractions at the concentration of 5 mg/L in the isolated ileum of guinea-pig. The administration of 15 mg/kg of AG 60 did not affect mean arterial blood pressure and heart rate in rat. AG 60 (15 mg/kg) given to anesthetized rabbits showed no effect on respiratory rate.

• 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.5 no.1
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• pp.74-81
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• 1997

DA-5018(N-(3-(3, 4-dimethylphenyl)propyl)-4-(2-aminoethoxy)-3-methoxyphenylacetamide) is a new capsaicin derivative under development as topical analgesic agent. The general pharmacological properties of DA-5018 on central nervous, cardiovascular, gastrointestinal and other organ systems were studied in experimental animals. DA-5018 cream (0.3%) had no effects on behavior, hexobarbital-induced sleeping time, body temperature, spontaneous activity, blood pressure, heart rate, intestinal charcoal propulsion, urine volume and electrolyte excretion even at a high dose of 2000 mg/kg in rats. In addition, DA-5Ol8 cream had little skin irritation compared to Zostrix-HP (capsaicin, 0.075%) cream in rabbits. In isolated guinea pig tissue studies, DA-5018 increased the contractility of trachea and ileum and also increased sinus rate of atrium in a range of 10^{-8}-10^{-5}$$ M, but its efficacy as a agonist was weak. These results suggest that DA-5018 cream might be used topically without serious side effects.