• Journal of Yeungnam Medical Science
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• v.6 no.2
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• pp.13-22
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• 1989

To investigate the effect of diazepam on the contractility of the intestinal smooth muscle, longitudinal muscle strip isolated from rat ileum was prepared for myography in isolated organ bath. 1) Basal tone of ileal muscle was reduced by diazepam concentration-dependently. 2) Higher concentrations(30 and 100 microM) of diazepam inhibited(p<0.05, p<0.001) the carbachol-induced contraction in a concentration-dependent manner ; but lower concentration of diazepam(10 microM) enhanced(p<0.05). 3) Histamine-induced contraction was inhibited by pretreatment with diazepam in a concentration-dependent manner. 4) $Ca^{++}$-induced tension recovery in calcium-free solution was inhibited in the presence of diazepam concentration-dependently. These results suggest diazepam reduces the contractility of the longitudinal muscle isolated from rat ileum via interference with influx of calcium into the muscle cells.

• YAKHAK HOEJI
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• v.37 no.6
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• pp.625-630
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• 1993

Among the six antihistamine agents tested in this study, homochlorcyclizine showed the highest bradykinin antagonistic activity in the receptor binding assay as well as the isolated rat ileum assay. Schild plot analysis of bradykinin-induced ileal contraction in the presence of three different concentrations of homochlorcyclizine revealed a pA$_{2}$=6.26, and a correlation coefficient of 0.984. Homochlorcyclizine of (100 $\mu{M}$ final concentration) also showed 25% antagonistic activity in the receptor binding assay.

• Biomolecules & Therapeutics
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• v.7 no.2
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• pp.170-177
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• 1999

PEG-hemoglobin SB1 (SB1), which is a hemoglobin-based oxygen carrier, is intended to use as a safe blood substitute against brain ischemia and stroke. The general pharmacological profiles of SB1 were studied. The doses given were 0, 5, 10, 20 ml/kg and drugs were administered intravenously. The animals used for this study were mouse, rat and guinea pig. SB1 showed no effects on general behavior, motor coordination, spontaneous locomotor activity, hexobarbital sleeping time, anticonvulsant activity, analgesic activity, blood pressure and heart rate, left ventricular peak systolic pressure, left ventricular end diastolic pressure, left ventricular developing pressure, double product, heart rate, coronary flow rate, smooth muscle contraction using guinea pig ileum, gastrointestinal transport, gastric secretion, urinary volume and electrolyte excretion at all doses tested except the decrease of body temperature. These findings demonstrated that SB1 possesses no general pharmacological effects at all doses tested.

• 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.

• The Korean Journal of Pharmacology
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• v.24 no.1
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• pp.103-109
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• 1988

Cyclobuxine D, extracted from Buxus microphylla var. koreana Nakai, is a steroidal alkaloid. Many pharmacological effects of cyclobuxine D were examined in our Lab. Cyclobuxine D showed a significant bradycardic effect in the rat heart and an inhibitory action on acetylcholine and $Ba^{++}-induced$ contraction of the longitudinal muscle isolated from the rabbit jejunum. In this study, we investigated the effect of cyclobuxine D on the contractile response-elicited by acetylcholine, oxytocin and $Ba^{++}$ in rat uterine. In order to analyse the inhibitory action of cyclobuxine D on the smooth muscle, we examined the inhibitory action of cyclobuxine D against the contractile response of the high potassium-depolarized rat ileum to calcium. Concentration-dependent decrease in the peak tension and duration of the acetylcholine, oxytocin and $Ba^{++}-induced$ contraction in the isolated rat uterus was observed when cyclobuxine D was added to the organ bath. The isolated longitudinal muscle from the rat ileum was immersed calcium-depleted potassium-depolarizing solution. Ten minutes after, 1.8 mM $CaCl_2$ was added to muscle bath and elicited a biphasic increase in muscle tension. Cyclobuxine D $(6.2{\times}10^{-5}\;M)$ produced an appreciable inhibition of both components of the mechanical response. In addition, $3.1{\times}10^{-4}\;M$ cyclobuxine D, introduced at a point when the tonic response had reached its maximum level, caused the muscle to exhibit a rapid lose of tension. Based on these experimental results, we propose the possibility that the inhibitory action of cyclobuxine D on the acetylcholine, oxytocin and $Ba^{++}-induced$ contraction in the isolated rat uterus may be due to blocking potassium-activated calcium channels, voltage-sensitive calcium channels.

• Korean Journal of Veterinary Research
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• v.42 no.2
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• pp.283-288
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• 2002

The present study was carried out to examine the effect of insulin formula on blood glucose change in normal Sprague-Dawley male rats. Also, this study was performed to investigate the feasibility of oral insulin formula development. To administrate the insulin formula into intestine, the surgical technique, celiotomy, was performed in rats. Insulin formula was administrated at a dose of 24.5 IU/kg via duodenum, ileum, and colon of the rats, and the blood glucose level was measured. For the comparison, the vehicle without insulin was administrated into ileum via celiotomy. Also, this insulin formula was administrated into rats orally using sonde and the same parameter was treasured. The bloods of all groups were collected from tail veins using syringes at given time interval. Orally administrated group did not show the change of blood glucose level and control group slightly show the change of blood glucose level at 1 hour after celiotomy. All intestinally administrated groups showed the change of blood glucose level. Among the tested groups, ileac administration group and colonic administration group showed the significant change of blood glucose level. Particularly, ileac administration group showed the lowest blood glucose level. To calculate the bioavailability of intestinal and oral administration, insulin solution was injected subcutaneosly, common insulin injection route, into another normal rats. The bioavailability of ileac group was 8.3% when compared with subcutaneous injection, duodenal group was 1.8%, colonic group was 4.2%, and oral group was 0.2%, respectively.

• YAKHAK HOEJI
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• v.40 no.5
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• pp.591-598
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• 1996

The water extracts of ten crude drugs were tested for the spasmolytic and anti-peptic ulcer activities on rat ileum smooth muscle contraction and aspirin-induced acute hemorrhag ic erosive gastritis respectively. The water extract of Aurantii immaturi pericarpium(AIP)($IC_{50}=1.5{\times}1O^{-2}$g/l), Aurantii nobilis pericarpium(ANP)($IC_{50}=2.5{\times}1O^{-2}$g/l), Cyperi rhizoma(CR)($IC_{50}=3.3{\times}1O^{-2}$g/l). Linderae radix(LR) ($IC_{50}=6.8{\times}1O^{-2}$), Aurantii fructus immaturus(AFI)($IC_{50}=11.8{\times}1O^{-2}$), Saussureae radix(SR)($IC_{50}=13.2{\times}1O^{-2}$g/l) and Ponciri fructus(PF)($IC_{50}=23.3{\times}1O^{-2}$g/l) showed inhibitory activity on the isometric contraction of rat ileum smooth muscle induced by electrical stimulation in a concentration-dependent manner, whereas the water extracts of Arecae pericarpium(AP), Agastachis herba(AH) and Magnoliae cortex(MC) potentiated the isometric contraction. In the aspirin-induced acute gastritis, the water extracts of MC, AP and CR reduced significantly the gastric juice secretion, gastric juice acidity and pepsin activity. They also showed protective activity of gastric mucosal layer from erosion and petichial hemorrhage in gross and histological examination.

• Journal of Pharmaceutical Investigation
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• v.21 no.4
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• pp.215-222
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• 1991

The absorption characteristics of itraconazole, which is an antifungal agent, from intestinal segments in the anesthetized rat i1l situ were investigated in order to design an effective oral drug delivery system. The pH-solubility profile of itraconazole, the rate and extent of absorption of itraconazole, the optimal absorption site(s) of itraconazole and the absorption enhancing effect of sodium cholate on itraconazole were examined in the present study. In situ single-pass perfusion method and recirculating perfusion technique using duodenum(D), jejunum(J) and ileum(I) were employed for the calculation of apparent permeability(Pe) and apparent first-order rate constant(Kobs). respectively. The results of this study were as follows; (1) Itraconazole showed appreciable aqueous solubility only at pH values of below 2.0. (2) pe(cm/sec) decreased in the following order: $D(10.24{\pm}1.78{\times}10^{-4})>J(8.86{\pm}0.79{\times}10^{-4})>I(3.78{\pm}0.13 X 10^{-4})$. (3) $Kobs(min^{-1})$ decreased in the following order: $J(17.12{\pm}3.19{\times}10^{-3})>D(13.37{\pm}0.6{\times}10^{-3})>I(11.05{\pm}0.91{\times}10^{-3})$. (4) The solubility of itraconazole markedly increased with the increase of the concentration of sodium cholate. (5) The addition of 10 mM sodium cholate significantly increased the apparent first-order rate constant of itraconazole in the ileum by a factor of 6.8.

• Journal of Physiology & Pathology in Korean Medicine
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• v.20 no.4
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• pp.924-928
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• 2006

This study was undertaken to determine the effects of Zusanli(ST 36) electro-acupuncture(EA) on the small intestinal motility in rat. The motor activity of the rat small intestine was evaluated by intestinal transfortation rate. Changes in the motility in vivo of ileum was measured before and 10 minutes after acupuncture. In order to examine whether EA effect was affected by stimulated duration and left or right sides of ST36 acupoint, both of the difference effects of left or right sides on acupoints of ST 36 and the stimulated duration of 10, 20, 30 min. were investigated on the motility in vivo of ileum. These results suggest that effect of Zusanli(ST36) for increasing the small intestinal motility should stimulate more than 20 minutes, left ST36 EA has stronger effect than right ST36 EA.

• Biomolecules & Therapeutics
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• v.18 no.4
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• pp.442-447
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• 2010

This study was conducted to determine whether treatment with the anti-inflammatory eupatilin influences intestinal smooth muscle contraction stimulated by carbachol and, if so, to investigate the related mechanism. Denuded ileal or colonic muscles from Sprague-Dawley rats were used for the study and measurements of isometric contractions were obtained using a computerized data acquisition system; this data was also combined with results from molecular experiments. Eupatilin from Artemisia asiatica Nakai significantly decreased carbachol-induced contractions in both ileal and colonic muscles. Interestingly, eupatilin decreased carbachol-induced phosphorylation of ERK1/2 more significantly than that of MYPT1 at Thr855 in ileal and colonic muscles. However, eupatilin significantly decreased phosphorylation of MYPT1 at Thr855, but only in ileal muscle. Therefore, thin filament regulation, including MEK inactivation and related phospho-ERK1/2 decrease, is mainly involved in the eupatilin-induced decrease of intestinal contraction induced by carbachol. In conclusion, this study provides the evidence and a possible related mechanism concerning the inhibitory effect of the flavonoid as an antispasmodic on the agonist-induced contractions in rat ileum and colonic muscles.