• Korean Journal of Fisheries and Aquatic Sciences
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• v.32 no.2
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• pp.232-237
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• 1999

The relationship between structure and contractile activity was studied on the three neuropeptide $\gamma$ (mammalian-, bowfin-, shark-NP$\gamma$) that were synthesized by the solid-phase method. Circular dichroism spectra showed that mammalian-, bowfin- and shark-neuropeptide $\gamma$ took an unordered structure in buffer solution and artificial liposome. The intestinal motility response was investigated with guinea-pig ileum, rat duodenum and carp intestine. In case of carp intestine, contractile activity was as follows; bowfin-NP$\gamma$> shark-NP$\gamma$>mammalian-NP$\gamma$, On the other hand, the contractile activity of mammalian-neuropeptide $\gamma$ was more potent than those of bowfin-, shark-neuropeptide $\gamma$ in the guinea-pig ileum and rat duodenum. These results suggest that NP$\gamma$ show the species-specific activity.

• Biomolecules & Therapeutics
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• v.10 no.4
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• pp.258-267
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• 2002

In this study the general pharmacological profiles of AS6 on the central nervous system, cardiovascular and the other organs were investigated. The dosages given were 0, 250, 500 and 1000 mg/kg and drugs were orally administered. The animals used for this study were mice, rats and guinea pigs. Significant increases (p<0.01) in the charcoal transport capacity were observed at the high dose of 1000 mg/kg and significant increases in retardation of pain threshold were observed in the test using acetic acid in all dosed animals. However, AS6 showed no noticeable effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital-induced sleep time, body temperature, analgesic activity in the test using hot plate method and anticonvulsant activity. Furthermore no noticeable effects were observed in cardiovascular functions in the isolated rat heart, contraction and relaxation of the smooth muscle in the isolated guinea ileum, gastric secretion and renal function.

• Journal of Physiology & Pathology in Korean Medicine
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• v.24 no.1
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• pp.143-151
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• 2010

In Vivo and In vitro antispasmodic effects of Jun-Si-Baek-Chul-San, a Traditional Korean Polyherbal Medicineconsisted of 7 types of herbs were observed in the present study. To clarify the effects of Jun-Si-Baek-Chul-San, on accelerating small intestinal movement induced by the stimulation of cholinergic neurotransmission, we evaluated the effects of Jun-Si-Baek-Chul-San on In vivo carbachol (an acetylcholinergic agent)-accelerated mice small intestinal transit and on In vitro contractions induced by low-frequency electrostimulation, KCl, histamine or acetylcholine using isolated guinea pig ileum. To induce the acceleration of mice small intestinal transit, Carbachol 1 mg/kg was once subcutaneously dosed 15min before last administration of the test drugs. In the present study, Jun-Si-Baek-Chul-San 500, 250 and 125 mg/kg or domperidone 20 mg/kg were orally pretreated on the carbachol-accelerated mice small intestinal transit once a day for 7 days and the small intestinal transit rateof activated charcoal powder were monitored. In vitro assays, Jun-Si-Baek-Chul-San1, 0.1, 0.01 and 0.001 mg/ml or domperidone $2{\times}10^{-5}M$ were treated 10min before ileal contraction was induced by filed stimulation, acetylcholine, KCl and histamine, and the % changes of contractions were observed compared to the treatment of inducer alone. In spontaneous contraction, the % changes of contractions were observed compared to treatment of vehicle alone at 10min after Jun-Si-Baek-Chul-San or domperidone treatment. The efficacy of Jun-Si-Baek-Chul-San was compared to those of domperidone. High concentration, 1 mg/ml of Jun-Si-Baek-Chul-San was found to decrease the spontaneous contraction of the isolated guinea-pig ileum. In addition, Jun-Si-Baek-Chul-San decrease contractions induced by electrostimulation, acetylcholine, histamine and KCl in the isolated guinea-pig ileum. In addition, Jun-Si-Baek-Chul-San effectively inhibited the accelerated small intestinal movement induced by carbachol stimulation of cholinergic neurotransmission in In vivo. Based on the results, although the exact molecular or action mechanism and which herbs or compound in Jun-Si-Baek-Chul-San are responsible for actions, it was concluded that Jun-Si-Baek-Chul-San normalization in the accelerated intestinal motility might be interfere with a variety of muscarinic, adrenergic and histaminic receptor activities or with the mobilization of calcium ions required for smooth muscle contraction non-specificly. Therefore, it is expected that Jun-Si-Baek-Chul-San will be promising as a prescription of clinical treatment of digestive tract disorders such as accelerated the motility of intestine, diarrhea or intestinal painful contractions.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.232.1-232.1
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• 2003

Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics and some active compounds such as FR 173657, LF 16-0687, and bradyzide were reported very recently. In our search for the new bradykinin antagonists, we designed to synthesize the analogues of FR173657 with two to three amide bonds and lipophilic ring system in each molecule. (omitted)

• Archives of Pharmacal Research
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• v.12 no.1
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• pp.22-25
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• 1989

Ethylacetate fraction from Orobanche crenata, contained two phenylpropanoid glycosides, exhibited some pharmacological properties. It was found to be non-toxic to rats in oral doses up to 500mg/100gm body weight. In large doses, it lowered the arterial blood pressure of anaethetised rats, and produced significant analgesic effect in mice and diuretic effect in rats. It further showed smooth muscle relaxant and antispasmodic effects in the isolated rabbit intestine and guinea-pig ileum respectively.

• Korean Journal of Pharmacognosy
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• v.17 no.3
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• pp.215-222
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• 1986

Although the 'Insamyangwee-tang' has been widely used in clinical purposes in the oriental medicine, its clinical efficacy is only documentated for the cases of gastritis, gastric ulcer and enteritis, but the experimental study on these has not been undertaken. So, to investigate the clinical efficacy of 'Insamyangwee-tang' comparing with animal experiments, This study was carried out. The results showed that relaxing action was shown on the isolated ileum in mice and that strong antagonistic actions were seen on $BaCl_2$, acetylcholine and histamine induced contraction of the ileum in mice, rats, rabbits and guinea-pigs that the relaxing effect of the intestinal smooth muscle was recognized. Inhibitory effects on transport rate in the small intestine of mice. Strong antagonistic actions were seen on acetylcholine induced contraction of duodenum in rats and remarkably inhibiting actions were seen of duodenum in rats. Inhibitory action on the secretion of gastric juice and pepsin, anti-ulceration effect was recognized.

• The Korean Journal of Pharmacology
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• v.30 no.2
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• pp.227-242
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• 1994

The general pharmacological effects of a new anthracycline anticancer agent, DA-125 $[7-0-(2,\;6-dideoxy-2-fluoro-{\alpha}-L-talopyranosyl)-adriamycinone-14-{\beta}-alaninate{\cdot}HCI]$ were investigated in mice, rats, guinea pigs, rabbits and dogs. Intravenous administration of DA-125 presented no significant effects on the central and peripheral nervous systems of ICR mice except a decrease in the numbers of acetic acid-induced writhing response at a dose of 10 mg/kg. In anesthetized rats and dogs, DA-125 produced a transient depression of blood pressure and an increase in heart rate, but did not affect the peripheral blood flow in the isolated ear vessels of rabbits and the mechanical functions of the isolated hearts of guinea pigs. No significant effects were observed on the gastrointestinal functions and the contractilities of smooth muscle preparations obtained from guinea pig trachea, rabbit ileum, pregnant and non-pregnant uterus and vas deferens of rats. DA-125 Increased the contractility of the isolated ileum of guinea pigs in a dose range of $10^{-6}{\sim}10^{-9}g/ml$, and also increased, but weaker than adriamycin, the vascular permeability in rat skin. DA-125 had no effect on the kallikrein-induced increase in permeability and the permeability of the visceral organs. DA-125 did not adversely affect the liver function and the blood coagulation system, and did not induce hemolysis in vitro. It is concluded from the results that the general pharmachological effects of DA-125 are similar to or weaker than those of adriamycin, and that little adverse effects are anticipated with a therapeutic dose range.

• Korean Journal of Pharmacognosy
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• v.20 no.3
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• pp.196-203
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• 1989

Experimental studies were conducted to investigate the effect of Sagan-Tang on analgesic, sedative, antipyretic, isolated ileum and blood vessel and so on. The results of this investigation were summarized as follows; Analgesic action by the acetic acid stimulating method in mice were recognized. Prolonging action against the hypnotic duration induced by thiopental-Na was noted in mice. Antipyretic effect in typhoid vaccine febrile rats was recognized. Spontaneous motility of the isolated ileum of mice was suppressed and contractions of the isolated ileum of mice and guinea-pig induced by accetylcholine chloride, barium chloride and histamine were remarkably inhibited. Vaso-diating and hypotensive actions were recognized in rabbits. GOT and GPT activities in the serum of rats damaged by $CCl_4$ and galactosamine were decreased remarkably.

• Archives of Pharmacal Research
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• v.15 no.1
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• pp.95-98
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• 1992

Alcoholic extract of seeds of Sesamum indicum (SI, 1-30mg/kg) caused hypotensive action in anesthetized rats. Heart rate was also decreased at slightly higher doses (10-30 mg/kg). Pretreatment with atropine (2 mg/kg) abolished these cardiovascular responses. In isolated spontaneously beating atria from guinea-pigs. SI caused decrease in force and rate of atrial contractions. In isolated guinea-pig ileum and rat uterus, SI (100-1000 ug/ml) produced contractile responses. All these actions of SI were abolished in the presence of atropine ($1\mu$M). These results indicate that alcoholic extract of seeds of Seamum indicum contains acetylcholine-like constituent(s) which explains some of the folkloric uses of plant.

• Biomolecules & Therapeutics
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• v.2 no.4
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• pp.347-360
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• 1994

The general and some pharmacological actions of DWP 301 were investigated in animals and the following results were obtained. In central nervous system, DWP 301 had no effects on the pentobarbital induced anaesthesia, rotarod test, traction test, analgesic action, anticonvulsant action in mice and body temperature in rat. But DWP 301 showed a little decrease of locomotor activity at a dose of 3,000 mg/kg. From these results, DWP 301 was considered to have little pharmacological effect on the central nervous system. Furthermore, DWP 301 had no influences on the normal blood pressure and heart rate. DWP 301 showed no effect on the isolated guinea pig ileum, trachea, right atrium, and nonpregnant rat uterus. But, in the isolated guinea pig vas deference, DWP 301 had showed inhibitory effect on the contractions produced by norepinephrine. DWP 301 showed rise of gastric juice pH and decrease of urine volume. Also, DWP 301 had no effect on the gastrointestinal motility and blood aggregation. From these results, it is concluded that the general pharmacological effect of DWP 301 are similar to or weaker than M and AGA.