• 대한수의학회지
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• 제38권4호
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• pp.730-736
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• 1998

To elucidate whether or not innervation of purinergic nerve and functional action of $P_{2X}$-, $P_{2Y}$-purinoceptor, the neurogenic effects of perivascular nerve stimulation were investigated using by physiograph recording system in isolated coronary artery of pig. 1. The contractile responses induced by perivascular nerve stimulation (20V, 0.5msec, 20sec) were the frequency (2~64Hz) dependent manner. 2. The neurogenic contractile responses induced by perivascular nerve stimulation were inhibited by the pretreatment with either ATP or adenosine ($10^{-7}{\sim}10^{-4}M$). 3. The neurogenic contractile responses induced by perivascular nerve stimulation (20V, 16Hz, 0.5msec, 20sec) were increased by the pretreatment with reactive blue 2, but were not affected by the pretreatment with 8-phenyltheopylline ($10^{-5}M$). 4. The neurogenic contractile responses induced by perivascular nerve stimulation (20V, 16Hz, 0.5msec, 20sec) were inhibited by the desensitization of the P2X-purinoceptor using by treatment of $10^{-5}M$, -methylene ATP as 3 times over again. The accomplished present study on isolated coronary artery of pig suggest that purinergic nerve is innervated and that the neurogenic contractile response was mediated by activation of $P_{2X}$-purinoceptor and the neurogenic relaxative response was mediated by activation of both $P_1$ and $P_{2Y}$-purinoceptor.

• The Korean Journal of Physiology and Pharmacology
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• 제21권4호
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• pp.407-413
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• 2017

Vascular reactivity can be influenced by the vascular region, animal age, and pathologies present. Prostaglandins (produced by COX-1 and COX-2) play an important role in the contractile response to phenylephrine in the abdominal aorta of young rats. Although these COXs are found in many tissues, their distribution and role in vascular reactivity are not clear. At a vascular level, they take part in the homeostasis functions involved in many physiological and pathologic processes (e.g., arterial pressure and inflammatory processes). The aim of this study was to analyze changes in the contractile response to phenylephrine of thoracic/abdominal aorta and the coronary artery during aging in rats. Three groups of rats were formed and sacrificed at three distinct ages: prepubescent, young and old adult. The results suggest that there is a higher participation of prostanoids in the contractile effect of phenylephrine in pre-pubescent rats, and a lower participation of the same in old rats. Contrarily, there seems to be a higher participation of prostanoids in the contractile response of the coronary artery of older than pre-pubescent rats. Considering that the changes in the expression of COX-2 were similar for the three age groups and the two tissues tested, and that expression of COX-1 is apparently greater in older rats, COX-1 and COX-2 may lose functionality in relation to their corresponding receptors during aging in rats.

• 대한약리학회지
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• 제12권1호
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• pp.45-55
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• 1976

The effect of positive inotropic agents on the contractile properties of myocardial muscle were studied in the cat papillary muscle preparation. For the purpose, the effects of ouabain $(1{\times}10^{-6}g/ml)$, norepinephrine (0.05r/m1) and Aconiti tuber butanol fraction (AF(5), $1{\times}10^{-4}$, $5{\times}10^{-4}$, $1{\times}10^{-3}$, $2{\times}10^{-3}g/ml$) on the contractile dynamics of the papillary muscle preparation isolated from right ventricle of cat were observed in terms of the characteristics of isometric twitch and the lengh-tension relation, the force-velocity relation and the load-extension relation of the series elastic component of contractile model of A.V. Hill. All the studied inotropic drugs similary increased the rate and the intensity of the developed isometric tension, while shortened the time from onset of contraction to peak tension and the total duration of contraction. In the afterloaded simultaneous isotonic and isometric contraction, they also similary increased the maximal velocity of shortening accompanied with the increasing the maximum developed force. In the load-extension relation all the drugs, however, had no appreciable influence on the properties of the series elastic component. Increasing the concentration, Aconiti tuber butanol fraction produced more pronounced effect on all the studied parameters of isometric and isotonic contraction of cat papillary muscle preparation. From the aspect of contractile dynamics, it seemed that the positive inotropic effect of ouabain, norepinephrine and Aconiti tuber butanol fraction are similary achieved through an influence on the behavior of the contractile component only.

• The Korean Journal of Physiology and Pharmacology
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• 제18권1호
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• pp.47-53
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• 2014

In this study, we propose that diprophylline exerts bidirectional modulation (BM) on the isolated rat jejunal segment depending on its contractile state. The results supported the hypothesis. Diprophylline ($20{\mu}M$) exerted stimulatory effects on the contractility of jejunal segment in six low contractile states while inhibitory effects in six high contractile states, showing the characteristics of BM. Diprophylline-induced stimulatory effect was significantly blocked by atropine, indicating the correlation with cholinergic activation. Diprophylline-induced inhibitory effect was partially blocked by phentolamine, propranolol, and L-N-Nitro-Arginine respectively, indicating their correlation with sympathetic activation and nitric oxide-mediated relaxing mechanisms. Diprophylline-induced BM was abolished by tetrodotoxin or in a $Ca^{2+}$ free condition or pretreated with tyrosine kinase inhibitor imatinib, suggesting that diprophylline-induced BM is $Ca^{2+}$ dependent, and that it requires the presence of enteric nervous system as well as pacemaker activity of interstitial cells of Cajal. Diprophylline significantly increased the reduced MLCK expression and myosin extent in constipation-prominent rats and significantly decreased the increased MLCK expression and myosin extent in diarrhea-prominent rats, suggesting that the change of MLCK expression may also be involved in diprophylline-induced BM on rat jejunal contractility. In summary, diprophylline-exerted BM depends on the contractile states of the jejunal segments, requires the presence of $Ca^{2+}$, enteric nervous system, pacemaker activity of interstitial cells of Cajal, and MLCK-correlated myosin phosphorylation. The results suggest the potential implication of diprophylline in relieving alternative hypo/hyper intestinal motility.

• Archives of Pharmacal Research
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• 제26권3호
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• pp.214-223
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• 2003

The present study was conducted to investigate the effects of green tea extract (GTE) on arterial blood pressure and contractile responses of isolated aortic strips of the normotensive rats and to establish the mechanism of action. The phenylephrine ($10^{-6}~10^{-5}M$)-induced contractile responses were greatly inhibited in the presence of GTE (0.3~1.2 mg/mL) in a dose-dependent fashion. Also, high potassium ($3.5{\times}10^{-2}~5.6{\times}10^{-2}{\;}M$)-induced contractile responses were depressed in the presence of 0.6~1.2 mg/mL of GTE, but not affected in low concentration of GTE (0.3 mg/mL). However, epigallocatechin gallate (EGCG, $4~12{\;}{\mu}g/mL$) did not affect the contractile responses evoked by phenylephrine and high $K^+$. GTE (5~20 mg/kg) given into a femoral vein of the normotensive rat produced a dose-dependent depressor response, which is transient. Interestingly, the infusion of a moderate dose of GTE (10 mg/kg/30 min) made a significant reduction in pressor responses induced by intravenous norepinephrine. However, EGCG (1 mg/kg/30 min) did not affect them. Collectively, these results obtained from the present study demonstrate that intravenous GTE causes a dose-dependent depressor action in the anesthetized rat at least partly through the blockade of adrenergic $\alpha_1$-receptors. GTE also causes the relaxation in the isolated aortic strips of the rat via the blockade of adrenergic $\alpha_1$-receptors, in addition to the unknown direct mechanism. It seems that there is a big difference in the vascular effect between GTE and EGCG.

• The Korean Journal of Physiology and Pharmacology
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• 제7권3호
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• pp.149-155
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• 2003

The aim of the present study was to examine the effects of platycodin D and $D_3$, which are active components derived from the roots of Platycodon grandiflorum A. DC., on the contractile force of the i3olated rat aorta and blood pressure of the anesthetized rat, and also to elucidate its mechanism of action. Both phenylephrine (an adrenergic ${\alpha}1$-receptor agonist) and high potassium (a membranedepolarizing agent) caused great contractile responses in the isolated aortic strips. Platycodin D at high concentration $(24{\mu}g/ml)$ inhibited contractile responses induced by phenylephrine $(10^{-5}\;M)$ and high potassium $(5.6{\times}10^{-2}\;M)$, while low concentrations of platycodin D $(4{\sim}8{\mu}g/ml$) did not affect those responses. However, platycodin $D_3\;(8{\sim}32{\mu}g/ml)$ did not alter the contractile responses evoked by phenylephrine and high $K^+$. Interestingly, the infusion of platycodin $D_3$ (1.0 mg/kg/30 min) significantly reduced the pressor responses induced by intravenous norepinephrine. However, platycodin $D_3$ (1.0 mg/kg/30 min) did not affect them. Taken together, these results show that intravenously administered platycodin D depresses norepinephrine-induced pressor responses in the anesthetized rat, at least partly through the blockade of adrenergic ${\alpha}1$-receptors. Platycodin D also caused vascular relaxation in the isolated aortic strips of the rat via the blockade of adrenergic ${\alpha}1$-receptors, in addition to an unknown direct mechanism. However, platycodin $D_3$ did not affect both norepinephrine-induced pressor responses and the isolated rat aortic contractile responses evoked by phenylephrine and high potassium. Based on these results, there seems to be much difference in the mode of action between platycodin D and platycodin $D_3$.

• 대한수의학회지
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• 제37권1호
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• pp.103-110
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• 1997

The experiments were carried out to elucidate the relationships between neurogenic effects of electrical transmural nerve stimulation and effect of adenosine 5'-triphosphate(ATP) to purinoceptor on the urinary bladder smooth muscle of pig. The results were as follows : 1. The contractile responses induced by electrical transmural nerve stimulation(10V or 20V, 0.5msec, 10sec) were the frequency(2~64Hz) dependent manner. 2. The contractile response induced by carbachol was responsed with a dose-dependent manner and the maximum contractility was $10^{-4}M$. 3. The contractile responses induced by ATP were increased in a dose-dependent manner ($10^{-5}{\sim}10^{-3}M$). 4. The contractile response induced by electrical transmural nerve stimulation(10V, 2~32Hz, 0.5msec, 10sec) was partially blocked by the treatment with atropine($10^{-5}M$), and was powerfully inhibited by 3 times of addition with ATP($10^{-5}M$). 5. The contractile response induced by electrical transmural nerve stimulation(10V, 2~32Hz, 0.5msec, 10sec) was partially blocked by the treatment with atropine($10^{-5}M$), and was completely blocked by the desensitization of the $P_{2X}$-purinoceptor using ${\alpha}$, ${\beta}$-methylene ATP($5{\times}10^{-5}M$). These results suggest that purinergic nerve was innervated, and ATP and acetylcholine was released by the electrical transmural nerve stimulation in urinary bladder smooth muscle of pig.

• 약학회지
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• 제29권4호
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• pp.199-205
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• 1985

It was previously reported that the deterioration rate of contractile force of the isolated heart from ginseng extract treated rat was slower than that from control. Present study was carried out to investigate the mechanism of the action of ginseng on the contractile force of the papillary muscle in terms of calcium metabolism. Rats weighing 200-300g were administered orally with ginseng ethanol extract (100mg/kg/day) for more than 10 days. The isolated papillary muscles from rat hearts were suspended in bath containing Krebs-Henseleit solution. When equilibration of contractile force of papillary muscle was reached, the rates of deterioration of contractile forces of papillary muscle from ginseng component treated rats were determined by washing with Ca-free Krebs-Henseleit solution and compared with that of normal hearts. At the beginning of washing, the rate of deterioration of contractile force of the papillary muscle was slower significantly in ginseng treated rats than in control rats, suggesting that calcium may be somehow involved in sustaining the contractility in ginseng treated hearts. Anoxia of papillary muscle with nitrogen gas to muscles inhibited the contractility, but differences between control and ginseng treated groups in the rate of deterioration were not observed. Influence of diltiazem, calcium blocker, on the contractility of papillary muscle from ginseng treated and control hearts was studied. Contractility of papillary muscle from control and ginseng treated hearts was inhibited by diltiazem in dose dependent manner but the inhibition of the ginseng treated muscles was much weak. The effect was significantly different. From the results, it seemed that slowing in deterioration rate of papillary muscle from ginseng treated hearts might be related to calcium which was mobilized from plasma membrane of internal organelle by ginseng.

• The Korean Journal of Physiology
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• 제22권1호
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• pp.31-39
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• 1988

This study was carried out to investigate the action of adenosine triphosphate (ATP) on the motility of immature pig uterine smooth muscle. ATP appeared contractile responses in a dose-dependent manner, showing the maximal contraction at the concentration of $10^{-3}M$ in the uterine smooth muscle strip. The contractile responses by $ATP(10^{-4}M)$ were not affected by atropine $(10^{-6}M)$, phentolamine $(10^{-6}M)$, propranolol $(10^{-6}M)$, pyrilamine $(10^{-6}M)$, cimetidine $(10^{-6}M)$, and theophyulline $(5{\times}10^{-5}M)$, but were inhibited uncompetitively by quinidine. The effects of these drugs on the contractile responses by prostaglandin $F_{2{\alpha}}(PGF_{2{\alpha}})$ were also comparable to those observed with ATP. When muscle strips were pretreated with indomethacin $(5{\times}10^{-5}M)$ for 20 min., the contractile responses by $ATP(10^{-4}M)$ were completely inhibited. But the contractile responses by $PGF_{2{\alpha}}$ were not affected by indomethacin. These results suggest that ATP elicited the contraction through noncholinergic- and nonadrenergic-receptor mediated by prostaglandin $F_{2{\alpha}}$ in pig uterine smooth muscle.

• The Korean Journal of Physiology and Pharmacology
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• 제16권6호
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• pp.437-446
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• 2012

Ulcerative colitis is an inflammatory bowel disease (IBD) characterized by recurrent episodes of colonic inflammation and tissue degeneration in human or animal models. The contractile force generated by the smooth muscle is significantly attenuated, resulting in altered motility leading to diarrhea or constipation in IBD. The aim of this study is to clarify the altered contractility of circular and longitudinal smooth muscle layers in proximal colon of trinitrobenzen sulfonic acid (TNBS)-induced colitis mouse. Colitis was induced by direct injection of TNBS (120 mg/kg, 50% ethanol) in proximal colon of ICR mouse using a 30 G needle anesthetized with ketamin (50 mg/kg), whereas animals in the control group were injected of 50% ethanol alone. In TNBS-induced colitis, the wall of the proximal colon is diffusely thickened with loss of haustration, and showed mucosal and mucular edema with inflammatory infiltration. The colonic inflammation is significantly induced the reduction of colonic contractile activity including spontaneous contractile activity, depolarization-induced contractility, and muscarinic acetylcholine receptor-mediated contractile response in circular muscle layer compared to the longitudinal muscle layer. The inward rectification of currents, especially, important to $Ca^{2+}$ and $Na^+$ influx-induced depolarization and contraction, was markedly reduced in the TNBS-induced colitis compared to the control. The muscarinic acetylcholine-mediated contractile responses were significantly attenuated in the circular and longitudinal smooth muscle strips induced by the reduction of membrane expression of canonical transient receptor potential (TRPC) channel isoforms from the proximal colon of the TNBS-induced colitis mouse than the control.