• Korean Journal of Pharmacognosy
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• v.19 no.4
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• pp.256-261
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• 1988

The present studies were investigated to find out the uterus contractive components and action mechanism of contractive components. We observed that the contractive components of Dianthi Herba were extracted with methanol and dissolved in butanol. The butanol extracts of Dianthi Herba increased uterus contractility, and fraction 2 obtained from butanol extract was more powerful than other fractions. This action was not blocked by atropine, papaverine, prazosin, propranolol, chlorpheniramine, methysergide and diltiazem in vitro.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1992.05a
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• pp.46-46
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• 1992

항궤양약 및 진경약의 효능을 검색할 수 있는 방법을 추구하는데 목적이 있다. 항궤양약의 약효는 Shay궤양, 수침 Stress궤양, indomethacin, histamine 및 prednisolone으로 유발된 궤양에 대하여 실시하였고 진경약의 효능은 흰쥐 fundus 절편을 이용한 in vitro 방법으로 실시하였다. 그 결과 항궤양약 효능시험은 shay 궤양에 있어서 omeprazole은 10mg/kg (i.d.)의 용량에서 유의성 있는 항궤양 효과를 나타내었으며, 수침 stress궤양에서 famotidine은 0.3mg/kg(p.o.), indomethacin 궤양에서 famotidine은 3mg/kg(p.o.), histamine궤양에서 cimetidine 은 50mg/kg(p.o.), prednisolone궤양에서 cimetidine은 1mg/kg(p.o.)의 용량에서 유의성 있는 효과를 나타내었다. 또한 진경약의 약효검색에 관하여는 세신(Asarum sieboldii)의 MeOH엑스가 흰쥐 위절편(fundus) 표본에서 비상경적 진정 작용이 있음을 확인하였고, 그 작용강도는 papaverine의 1/50에 해당되나 이를 분획하였을 경우에 hexane 분획에서 papaverine의 1/2에 해당하는 강도가 있다는 결과를 얻었다.

• Clinical and Experimental Reproductive Medicine
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• v.13 no.2
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• pp.181-185
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• 1986

To estimate the penile blood flow changes during artificial with erection intracorporeal papaverine injection, we injected 99 m Technitium-Human Serum Albumin via antecubital vein simultaneously and calculate the radioisotope activity of the penis using computerized Gamma Camera. We classified the results into 3 groups according to the transit time, erection persistent time and venous index in 67 impotence patients. We defined the arteriogenic impotence with the delayed transit time (more than 600 seconds) in 13 patients and venogenic with the shortened erection persistant time (less than 200 seconds) and decreased venous index (less than 0.8) in 11 patients. The rest of them (43 patients) were regarded as equivocal impotence, probably nonvasculogenic or psychogenic.

• Biomolecules & Therapeutics
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• v.29 no.3
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• pp.295-302
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• 2021

Microglial priming is the process of microglial proliferation and activation in response to neurodegeneration and abnormal protein accumulation. Priming makes microglia susceptible to secondary inflammatory stimuli and causes exaggerated inflammatory responses. In the present study, we established a microglial priming model in mice by administering a single injection of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP, 20 mg/kg). MPTP induced microglial activation without dopaminergic degeneration; however, subsequent treatment with a sub-toxic dose of lipopolysaccharides (LPS) induced an amplified inflammatory response and caused nigrostriatal dopaminergic degeneration. These pathological and inflammatory changes, including microglial activation and dopaminergic cell loss in the substantia nigra (SN) area were reversed by papaverine (PAP) administration. In addition, MPTP/LPS enhanced interleukin-1β (IL-1β) expression and processing via nod-like receptor protein 3 (NLRP3) inflammasome activation in the SN region of mice. However, PAP treatment suppressed inflammasome activation and subsequent IL-1β maturation. Moreover, PAP inhibited nuclear factor-κB (NF-κB) and enhanced cAMP-response element binding protein (CREB) activity in the SN of MPTP/LPS mice. These results suggest that PAP inhibits the activation of NLRP3 inflammasome by modulating NF-κB and CREB signaling pathways, which results in reduced microglial activation and neuronal cell death. Thus, PAP may be a potential candidate for the treatment of Parkinsons's disease, which is aggravated by systemic inflammation.

• Journal of Chest Surgery
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• v.37 no.10
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• pp.839-844
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• 2004

Background: The Y-composite graft of internal thoracic artery and radial artery is commonly used in coronary bypass surgery. The aim of this study is to look for a way to raise the free flow of the internal thoracic graft and to see flow dynamics of the Y-graft. Material and Method: In 15 patients undergoing coronary bypass surgery, free flow of the in-situ internal thoracic artery graft was measured using two different papaverine application methods; extraluminal papaverine spray in 7 patients and intraluminal papaverine injection in 8. In 18 other patients for whom the Y-graft was used, total free flow and flow changes from the two ends were measured. Result: The free flow of the in-situ internal thoracic artery graft almost doubled with internal papaverine injection than with external papaverine spray $(47.7\pm9.6$ mL/min $vs.100.8\pm26.3$ mL/min, p<0.001). Total flow of the Y-composite graft was significantly more than either flow of the internal thoracic artery end or radial artery graft end $(173.3\pm45.3$ mL/min vs. $121.1\pm34.3$ mL/min or $117.5\pm42.8$ mL/min). When both ends of the Y-composite graft were opened, free flows from the two ends were similar $(85.4\pm27.8$ mL/min vs: $87.9\pm42.4$ mL/min, p=0.772). The flow of one end of the Y-composite graft was increased significantly by clamping of the other-end than when both ends were opened. Conclusion: Intraluminal papaverine injection is very effective in raising free flow of the internal thoracic artery graft, and the free flow of the Y-composite graft of in-situ internal thoracic artery and free radial artery graft is more than that of the in-situ internal thoracic artery graft. The flow of one end flow of the Y-graft may be altered by the flow change of the other end.

• Tuberculosis and Respiratory Diseases
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• v.39 no.6
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• pp.474-483
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• 1992

Background: Regardless of its causes, acute lung injury is characterized pathophysiologically by increased pulmonary arterial pressure and the protein-rich edema. Many inflammatory mediators are known to be involved in the pathogenesis of acute lung injury, including oxygen free radicals (OFR). But the changes in pulmonary capillary pressure in the OFR-induced acute lung injury is not clear. While the pulmonary edema characterized by the movement of fluid and solutes is dependent on the pressure gradient and the alveolar-capillary permeability, the role of pulmonary capillary pressure in the development of pulmonary edema is also not well understood. Method: Male Sprague-Dawley rats were divided into 5 groups: normal control (n=5), xanthine/xanthine oxidase (X/XO)-treated group (n=7), catalase-pretreated group (n=5), papaverine-pretreated group (n=7), and indomethacin-pretreated group (n=5). In isolated perfused rat lungs, the sequential changes in pulmonary arterial pressure, pulmonary capillary pressure by double occlusion method, and lung weight as a parameter of pulmonary edema were determined. Results: Pulmonary arterial pressure and pulmonary capillary pressure were increased by X/XO. This increase was significantly attenuated by catalase and papaverine, but indomethacin did not prevent the X/XO-induced increase. Lung weight gain was also observed by X/XO perfusion. It was prevented by catalase. Papaverine did not completely block the increase, but significantly delayed the onset. Indomethacin had no effect on the increase in lung weight. Conclusion: These data suggest that increased pulmonary capillary pressure by OFR may aggravate pulmonary edema in the presence of increased alveolar-capillary permeability and this may not be mediated by cyclooxygenase metabolites.

• Journal of Chest Surgery
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• v.18 no.4
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• pp.732-739
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• 1985

This study was experimentally undertaken to evaluate the effect of the coronary vasodilator-mixed cardioplegic solution on myocardial protection during prolonged aortic cross-clamping. The dogs were divided into two groups: control group A[received hypothermic cardioplegic solution without any additive coronary vasodilator], and comparing group 8[received hypothermic cardioplegic solution, mixed with various coronary vasodilators and Inderal]. Group A further was divided into two subgroups: subgroup A-1[ischemic time, 90 minutes], and subgroup A-2 [ischemic time, 240 minutes]. Group B further was divided into five subgroups: subgroup B-1 [received papaverine mixed hypothermic cardioplegic solution], subgroup B-2[received nitroglycerin mixed hypothermic cardioplegic solution], subgroup B-3 [received nitroprusside mixed hypothermic cardioplegic solution, subgroup B-4[received hydralazine mixed hypothermic cardioplegic solution], and subgroup B-5 [received inderal mixed hypothermic cardioplegic solution]. The specimens from all of the subgroups were studied by electron microscopic examination. The specimens of subgroups [B-l, B-2 8-3, and B-4], received coronary vasodilators mixed hypothermic cardioplegic solutions, were also compared by methylene blue induced staining of the myocardium and coronary vessels. The results obtained were as followings: l. On electron microscopic examination, all of the specimens, including subgroup A-2, showed no irreversible change of the myocardium. But the best result was obtained from the subgroup B-l, treated by papaverine mixed hypothermic cardioplegic solution. The subgroup B-2, treated by nitroglycerin, was next. And the subgroup B-5, treated by Inderal, was agreeable, comparing the electron microscopic finding with control group in the effect of myocardial protection. 2. The distribution in the myocardium of cardioplegic solution was demonstrated with the aid of methylene blue staining in the subgroups of B-l, B-2, B-3, and B-4, and they were the groups treated by papaverine, nitroglycerin, nitroprusside, and hydralazine in their grouping order. The best result was obtained from the subgroup B-1 [papaverine]. The subgroup B-2 [nitroglycerin] was next. The subgroup B-3 [nitroprusside] was moderate in finding of the colorization. The subgroup B-4 [hydralazine] was the poorest in the distribution of the cardioplegic solution in the myocardium. From these results, it appeared that myocardial protection during ischemic arrest for open heart surgery could be enhanced considerably when coronary dilatation was assured.

• Biomedical Science Letters
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• v.11 no.4
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• pp.435-439
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• 2005

To determine the appropriate concentration of papaverine hydrochloride(PPV) for therapeutic intraarterial infusion against cerebral vasospasm and to measure the mean blood flow velocity of the middle cerebral artery in rabbits. Vasospasm was induced in the experimental groups (3 days after infusion; group 1, n=3, 7 days after infusion; group 2, n=3) and a control group (n=l) by placing a blood clot in the subarachnoid space around the top of the internal carotid siphon. PPV (5 mg/kg) was infused into the internal carotid artery. The vascular diameters of the internal carotid artery (ICA) and middle cerebral artery (MCA) were measured on angiograms before and after infusion. The mean blood flow velocity in the MCA was measured on transcranial doppler sonograms before and 24 hours after infusion. After fixation, the MCA was dissected out, stained, and examined microscopically. After PPV infusion in both groups, vascular dilatation of about $20\%$ was seen. The mean increase in blood flow velocity in the group $1(30\%)$ was smaller than in the group $2(70\%)$. The mean blood flow velocity in the MCA decreased by about $30\%$ in both groups, but increased again after 24 hours nearly to the level before PPV infusion. PPV infusion may be more effective in early stages of vasospasm when vascular walls have fewer histologic changes.

• The Korean Journal of Pharmacology
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• v.10 no.1 s.15
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• pp.47-52
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• 1974

The isolated rabbit gall bladder strips were prepared according to the technique described by Amer and Becvar (1969). The strips were placed in a bath containing 100 ml of Locke-Ringer solution maintained at $38^{\circ}C$. Oxygen was continuously bubbled through the solution. The tension of the muscle strip was initially adjusted to 0.7g. The contractile response was measured isometrically by a force-displacement transducer connected to a polygraph. The effect of a number of autonomic drugs were studied for their interaction with caerulein (Prof. V. Erspamer, F.I. 6934 Caerulein, Farmitalia, Italia), a gastrin or CCK.PZ like peptide, on isolated rabbit gall bladder strips. In this preparation caerulein produced contractions of CCK-PZ type, but the relative potency on a weight basis was 40 times that of CCK-PZ. The response of caerulein was not modified by either cholinergic or alpha or beta adrenergic blockade. However, the response of caerulein and of barium on the strips were prevented by papaverine or aminophylline. Isoproterenol, papaverine or aminophylline alone relaxed the preparation whereas caerulein, CCK-PZ, acetylcholine, serotonin, histamine or barium chloride contracted the preparation. In summary, it is concluded that caerulein on the gall bladder strip seems to act independently of the autonomic nervous system and mediated via mechanisms apparently similar to those involved in the action of barium chloride.

• Journal of Microbiology
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• v.38 no.4
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• pp.255-259
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• 2000

For rapid and sensitive measurement of antiviral activities, application of a recombinant virus containing firefly luciferase gene was attempted. Recombinant human cytomegalovirus (HCMV) containing luciferase gene driven by HCMV late gene pp28 promoter (HCMV/pp28-luc) was used to test the antiviral activities of three known compounds and the result was compared with results from the conventional plaque assay for measuring the production of infectious viruses. When human fibroblast cells were infected with HCMV/pp28-luc, luciferase activity was observed at 2 days after infection and reached maximum at 6 days after infection, whereas the production of infectious virus was maximal at 4 days after infection. The antiviral activities of ganciclovir, acyclovir, and papaverine were measured in HFF cells infected with HCMV/PP28-luc and the luciferase activity was compared with the infectious virus titers. Luciferase activity decreased as the concentration of ganciclovir or papaverine increased, while there was a slight decrease in luciferase activity with acyclovir. The level of the decrease in Luciferase activity was comparable to the level of decrease in the production of infectious virus. Therefore, the antiviral assay using recombinant virus HCMV/pp28-luc resulted in sensitivity similar to the conventional plaque assay with a significant reduction in assay time.