Polish journal of pharmacology最新文献

Hypoxic and pharmacological preconditioning preserves vasomotor response of porcine coronary artery. 缺氧和药物预处理保留了猪冠状动脉的血管舒缩反应。

Polish journal of pharmacology Pub Date : 2004-11-01

Jernej Kuzner, Gorazd Drevensek, Borut Gersak, Metka Budihna

{"title":"Hypoxic and pharmacological preconditioning preserves vasomotor response of porcine coronary artery.","authors":"Jernej Kuzner, Gorazd Drevensek, Borut Gersak, Metka Budihna","doi":"","DOIUrl":"","url":null,"abstract":"Vasomotor response of the coronary artery depends on both endothelial and smooth muscle cells. Response is altered by hypoxia-reoxygenation-induced damages. Hypoxic preconditioning and pharmacological preconditioning as well can prevent these alterations. We compared the effectiveness of both types of preconditioning against hypoxia-reoxygenation-induced changes in vasomotor response of the isolated artery. Porcine arterial rings (3-4 mm wide) were cut from the left anterior descending porcine coronary artery and placed in Krebs-Henseleit solution. In order to obtain control response of the arteries, we contracted arterial rings with 20 mM KCl before (\"standard contraction\") and after 60-min hypoxia and 30-min reoxygenation. In other groups, nitric oxide-synthase and cyclooxygenase were inhibited. Then, the rings were pre-contracted with U46619 and relaxed by cumulative addition of the substance P. Contractions and relaxations of non-preconditioned and hypoxically or pharmacologically preconditioned rings were compared. Hypoxic preconditioning was performed by two periods of 5-min hypoxia and 10-min reoxygenation. For pharmacological preconditioning, we used application of adenosine, adrenaline, acetylcholine and angiotensin II. Analysis was performed with one-way ANOVA, followed by Dunnett's Multiple Comparison Test. After hypoxia-reoxygenation, in non-preconditioned rings KCl-induced contractions were significantly increased compared to standard contraction. Relaxations of hypoxically and pharmacologically preconditioned rings (expressed as percentages of U46619-induced pre-contraction) were significantly decreased (p < 0.01) compared to hypoxic but not to normoxic rings. Hypoxic and pharmacological preconditioning may preserve contraction and endothelium-dependent relaxation of porcine coronary artery after long-lasting hypoxia-reoxygenation.","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"789-97"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24916272","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Changes and their regression in the osseous system in rats after administering a cytostatic drug inhibiting tumor cell division in the phase of DNA synthesis. 给药抑制肿瘤细胞在DNA合成阶段分裂后大鼠骨系统的变化及其消退。

Polish journal of pharmacology Pub Date : 2004-11-01

Urszula Cegieła, Maria Pytlik, Waldemar Janiec

{"title":"Changes and their regression in the osseous system in rats after administering a cytostatic drug inhibiting tumor cell division in the phase of DNA synthesis.","authors":"Urszula Cegieła, Maria Pytlik, Waldemar Janiec","doi":"","DOIUrl":"","url":null,"abstract":"Chemotherapeutic drugs may disturb the bone tissue metabolism and cause osteopenia, however, the pathomechanism of the damaging effect of cytostatics on this tissue has not been well recognized so far. The detrimental effect may result from a direct cytotoxic action of these drugs on cells remodeling the bone, or on osteogenic cells present in the bone and in the bone marrow, or may be the result of hormonal disorder caused by impaired function of gonads. The aim of this study was to investigate the in vivo effect of 5-fluorouracil (5-FU), a cytostatic agent which inhibits tumor cell division in the phase of DNA synthesis, on the bone remodeling in rats and to examine whether the period of 4 weeks was sufficient for regression of changes elicited by administering 5-FU. Changes in the bone tissue following administration of 5-FU and their regression were evaluated by assessing macrometric and histomorphometric parameters as well as of mechanical properties of the femur. The tests were carried out on male Wistar rats. 5-FU was administered at the doses: 30 mg/kg per os (po) daily for 5 days every 2 weeks; 15 mg/kg im daily for 5 days every 2 weeks; 65 mg/kg im once weekly. Changes in the osseous tissue were examined 4 weeks after the first dose of 5-FU administration. Regression of the changes was examined 8 weeks after the first dose of 5-FU administration (the 5-FU was not administered between 30th and 57th day after the first dose of 5-FU administration). As a result of our research, it was established that 5-FU disturbed the bone remodeling processes in rats, mostly by impairing the process of new bone matrix synthesis, which leads to impaired mineralization process and decreased mechanical endurance of the femur. It was also established that the period of 4 weeks was not sufficient for regression of the changes in the osseous tissue caused by 5-FU administration.","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"805-16"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24916275","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Chronic treatment with citalopram does not affect the expression of alpha1-adrenergic receptor (alpha1-AR) subtypes. 慢性西酞普兰治疗不影响α 1-肾上腺素能受体(α 1- ar)亚型的表达。

Polish journal of pharmacology Pub Date : 2004-11-01

Grzegorz Kreiner, Adam Bielawski, Agnieszka Zelek-Molik, Marta Kowalska, Irena Nalepa

引用次数: 0

Intraamygdaloid administration of BIBO 3304 increases water intake and extends anxiolytic effects. 杏仁核内给药BIBO 3304可增加水分摄入并延长抗焦虑作用。

Polish journal of pharmacology Pub Date : 2004-11-01

Joanna M Wierońska, Katarzyna Stachowicz, Aleksandra Kłodzińska, Maria Smiałowska, Andrzej Pilc

引用次数: 0

Effects of joint administration of imipramine and amantadine in patients with drug-resistant unipolar depression. 丙咪嗪和金刚烷胺联合应用对耐药单极抑郁症患者的影响。

Polish journal of pharmacology Pub Date : 2004-11-01

Zofia Rogóz, Marta Dziedzicka-Wasylewska, Władysława A Daniel, Jacek Wójcikowski, Dominika Dudek, Andrzej Wróbel, Andrzej Zieba

{"title":"Effects of joint administration of imipramine and amantadine in patients with drug-resistant unipolar depression.","authors":"Zofia Rogóz, Marta Dziedzicka-Wasylewska, Władysława A Daniel, Jacek Wójcikowski, Dominika Dudek, Andrzej Wróbel, Andrzej Zieba","doi":"","DOIUrl":"","url":null,"abstract":"The paper describes the effect of amantadine (AMA) supplementation on imipramine (IMI) therapy in patients (with treatment-resistant unipolar depression) who fulfilled DSM IV criteria for major depression. Twelve patients were enrolled to the study on the basis of history of their illness and therapy. Following 2 weeks of washout period, the patients were treated with IMI twice daily (100-150 mg/day) for 6 weeks, and then AMA was introduced (twice daily, 100-150 mg/day) and administered jointly with IMI for further 6 weeks. Thereafter, AMA was withdrawn, and the patients were treated with IMI alone for 2 weeks. Hamilton Depression Rating Scale (HDRS) and Beck Depression Inventory (BDI) were used to assess efficacy of antidepressant therapy. IMI changed neither HDRS nor BDI score after 3 or 6 weeks of treatment when compared with washout (before treatment). AMA supplementation significantly reduced both HDRS and BDI scores after 3- or 6-week supplementation. AMA augmentation of IMI treatment was beneficial and lasted even after AMA withdrawal. Moreover, pharmacokinetic data indicate that AMA did not influence significantly the plasma concentration of the IMI and its metabolite, desipramine, in the patients during joint treatment with AMA and IMI, what suggests the lack of pharmacokinetic interaction. These results suggest that joint therapy with IMI and AMA may be successful in the treatment-resistant unipolar depression.","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"735-42"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25084669","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

New 4-[omega-(diarylmethylamino)alkyl]- and 4-[omega-(diarylmethoxy)alkyl]-1-arylpiperazines as selective 5-HT1A/5-HT2A receptor ligands with differentiated in vivo activity. 新的4-[欧米伽-(二芳基甲基胺)烷基]-和4-[欧米伽-(二芳基甲氧基)烷基]-1-芳基哌嗪作为选择性5-HT1A/5-HT2A受体配体具有分化的体内活性。

Polish journal of pharmacology Pub Date : 2004-11-01

Maria H Paluchowska, Sijka Charakchieva-Minol, Ewa Tatarczyńska, Aleksandra Kłodzińska, Katarzyna Stachowicz, Ewa Chojnacka-Wójcik

{"title":"New 4-[omega-(diarylmethylamino)alkyl]- and 4-[omega-(diarylmethoxy)alkyl]-1-arylpiperazines as selective 5-HT1A/5-HT2A receptor ligands with differentiated in vivo activity.","authors":"Maria H Paluchowska, Sijka Charakchieva-Minol, Ewa Tatarczyńska, Aleksandra Kłodzińska, Katarzyna Stachowicz, Ewa Chojnacka-Wójcik","doi":"","DOIUrl":"","url":null,"abstract":"Two series of novel 4-ethyl- or 4-propyl-1-arylpiperazines (5-12) with the 4,4'-disubstituted diphenylmethylamino (series a) or the diphenylmethoxy (series b) terminal fragment were synthesized and evaluated for their binding affinity at 5-HT1A and 5-HT2A receptors. The influence of the introduction of 4-methyl, 4-chloro or 4-fluoro substituents at both phenyl rings of that terminal moiety on in vitro and in vivo 5-HT1A receptor activity of those modified compounds was discussed. Compounds 5a, 6a, 9a-12a, 5b, 6b, 9b, 11b and 12b displayed high to fairly high affinity for 5-HT1A receptors (Ki = 2.4-72 nM). Compounds of both series showed low or very low 5-HT2A receptor affinity (Ki = 155-5400 nM). Amines 5a, 6a, 11a, and their ether analogs 5b, 6b and 11b, also possessed high or moderate alpha(1)-adrenoceptor affinity (K(i) = 6-104 nM). The functional activity of compounds 5a, 6a, 9a-12a, 5b, 8b, 9b, 11b and 12b was tested in vivo in the commonly used animal models. The majority of those ligands behaved like 5-HT1A receptor antagonists, their influence on the pre- and/or postsynaptic sites being diverse, though. They exhibited characteristics of partial agonists of postsynaptic 5-HT1A receptors (11a), of weak antagonists of pre- and postsynaptic sites (12a, 9b), of antagonists of presynaptic (5a) or of antagonists of postsynaptic 5-HT(1A) receptors (9a, 10a, 5b, 8b, 11b and 12b) while, 6a was devoid of functional activity at those receptors. The above findings indicate that introduction of 4-methyl, 4-chloro or 4-fluoro substituents to the diphenylmethyl part of the 1-(2-methoxyphenyl)piperazines tested in vivo may modify their 5-HT1A receptor functional activity.","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"743-54"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25084670","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Antiarrhythmic profile and endothelial action of novel decahydroquinoline derivatives. 新型十氢喹啉衍生物的抗心律失常特征和内皮作用。

Polish journal of pharmacology Pub Date : 2004-11-01

Valery I Kozlovski, Vladimir P Vdovichenko, Stefan Chlopicki, Sergey S Malchik, Kaldybek D Praliyev, Oral T Zcilkibayev

{"title":"Antiarrhythmic profile and endothelial action of novel decahydroquinoline derivatives.","authors":"Valery I Kozlovski, Vladimir P Vdovichenko, Stefan Chlopicki, Sergey S Malchik, Kaldybek D Praliyev, Oral T Zcilkibayev","doi":"","DOIUrl":"","url":null,"abstract":"We tested antiarrhythmic and endothelial action of novel decahydroquinoline derivatives. Antiarrhythmic activity was analyzed using models of aconitine-, calcium chloride-, and adrenaline-induced arrhythmias in rats. Potency to induce nitric oxide (NO)-dependent coronary vasodilation was assessed in isolated guinea pig heart perfused according to Langendorff technique. Among 15 novel decahydroquinoline derivatives (D1-15), four of them displayed antiarrhythmic activity (D12-D15). D12-D15 compounds were more active in the model of aconitine-induced arrhythmias than in calcium chloride-induced arrhythmias and were inactive in the model of adrenaline-induced arrhythmias. Profile of antiarrhythmic activity of D12-D15 compounds was similar to that of quinidine and procainamide. Interestingly, in the isolated guinea pig heart D14 and D15 (10(-5) M) induced coronary vasodilation, that was mediated by endothelium-derived NO. In conclusion, novel decahydroquinoline derivatives described here (D12-D15) show antiarrhythmic activity typical of antiarrhythmic drugs of class I. Importantly, some of these compounds (D14, D15) release NO from coronary endothelium, which may provide an additional therapeutic benefit.","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"767-74"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25084672","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Inhibition of rodent brain monoamine oxidase and tyrosine hydroxylase by endogenous compounds - 1,2,3,4-tetrahydro-isoquinoline alkaloids. 内源性化合物- 1,2,3,4-四氢异喹啉生物碱对鼠脑单胺氧化酶和酪氨酸羟化酶的抑制作用。

Polish journal of pharmacology Pub Date : 2004-11-01

Antoni Patsenka, Lucyna Antkiewicz-Michaluk

引用次数: 0

Effect of imipramine treatment on plasma dopamine beta-hydroxylase activity in chronic mild stress in rats. 丙咪嗪治疗对慢性轻度应激大鼠血浆多巴胺-羟化酶活性的影响。

Polish journal of pharmacology Pub Date : 2004-11-01

Mariola Grabowska, Małgorzata Schlegel-Zawadzka, Mariusz Papp, Gabriel Nowak

引用次数: 0

Role of adrenal gland hormones in the mechanism of antiulcer action of nimesulide and ranitidine. 肾上腺激素在尼美舒利和雷尼替丁抗溃疡作用机制中的作用。

Polish journal of pharmacology Pub Date : 2004-11-01

Halis Süleyman, Berna Demircan, Fatma Göçer, Zekai Halici, Ahmet Hacimüftüoğlu

{"title":"Role of adrenal gland hormones in the mechanism of antiulcer action of nimesulide and ranitidine.","authors":"Halis Süleyman, Berna Demircan, Fatma Göçer, Zekai Halici, Ahmet Hacimüftüoğlu","doi":"","DOIUrl":"","url":null,"abstract":"In the present study, we investigated whether the antiulcer effects of nimesulide (100 mg kg(-1) and ranitidine (150 mg kg(-1) were dependent on the adrenal cortex hormones. The antiulcer effects of nimesulide and ranitidine were examined in the indomethacin-induced gastric ulcer model in rats (first experiment). The mean ulcer areas in the control and ranitidine-treated groups were 11.1 +/- 3.18, 1.4 +/- 1.11 mm2, respectively. There was not any gastric damage in nimesulide-treated group. The mean ulcer area of control group (second experiment) administered metyrapone and indomethacin was 11.8 +/- 9.9, and it measured 2.0 +/- 1.41 mm2 in ranitidine-given group, while gastric damage was not observed in nimesulide-administered group. In adrenalectomized and indomethacin-treated rats (third experiment), the mean ulcer area was 17.9 +/- 11.5 mm2 in the nimesulide group, gastric ulcer was not seen in ranitidine group. In adrenalectomized rats (fourth experiment), the mean ulcer areas were 29 +/- 14.3, 23 +/- 11.2 and 1.3 +/- 2.4 mm2 in control group given indomethacin, only nimesulide or indomethacin + ranitidine, respectively. The obtained results indicated that adrenal cortex hormones played a role in antiulcer effect of nimesulide, but not ranitidine.","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"799-804"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24916273","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0