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Polish journal of pharmacology最新文献

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Effect of administration of alendronate sodium and retinol on the mechanical properties of the femur in ovariectomized rats. 阿仑膦酸钠和视黄醇对去卵巢大鼠股骨力学性能的影响。
Polish journal of pharmacology Pub Date : 2004-11-01
Leszek Sliwiński, Waldemar Janiec, Maria Pytlik, Joanna Folwarczna, Ilona Kaczmarczyk-Sedlak, Wojciech Pytlik, Urszula Cegieła, Barbara Nowińska
{"title":"Effect of administration of alendronate sodium and retinol on the mechanical properties of the femur in ovariectomized rats.","authors":"Leszek Sliwiński,&nbsp;Waldemar Janiec,&nbsp;Maria Pytlik,&nbsp;Joanna Folwarczna,&nbsp;Ilona Kaczmarczyk-Sedlak,&nbsp;Wojciech Pytlik,&nbsp;Urszula Cegieła,&nbsp;Barbara Nowińska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Alendronate sodium, an aminobisphosphonate with potent antiresorptive activity, is used in the treatment of postmenopausal osteoporosis. Retinol, as a component of multivitamin preparations, is frequently used especially by elderly people. There are no reports on the interaction of alendronate sodium and retinol. The aim of the present study was to investigate the effect of administration of alendronate sodium and retinol on mechanical properties of the femoral bone in bilaterally ovariectomized rats. The experiments were carried out on 3-month-old Wistar rats, divided into 7 groups: I - sham-operated control rats, II - ovariectomized control rats, III - ovariectomy + alendronate sodium 3 mg/kg po, IV - ovariectomy + retinol 700 IU/kg po, V - ovariectomy + retinol 3500 IU/kg po, VI - ovariectomy + alendronate sodium 3 mg/kg po + retinol 700 IU/kg po, VII - ovariectomy + alendronate sodium 3 mg/kg po + retinol 3500 IU/kg po. The drugs were administered to the rats daily by oral gavage for 28 days. Body mass gain, bone mass, bone mineral content and calcium content in the femur and L-4 vertebra and mechanical properties of the whole femur (extrinsic stiffness, ultimate load, breaking load, deformation caused by the ultimate load) and the neck of the femur (load at fracture), were examined. Bilateral ovariectomy induced osteopenic changes in the rat skeletal system. Alendronate sodium (3 mg/kg po) counteracted the development of osteopenia induced by ovariectomy. Retinol at both used doses unfavorably affected the examined bone parameters of ovariectomized rats. Retinol administered with alendronate sodium lessened the preventive action of alendronate on the development of osteopenic changes in the skeletal system of ovariectomized rats.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"817-24"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24916276","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
Introduction of a new complex imide system into the structure of LCAPs. The synthesis and a 5-HT1A, 5-HT2A and D2 receptor binding study. 在lcap结构中引入一种新的复杂亚胺体系。5-HT1A、5-HT2A与D2受体结合的研究。
Polish journal of pharmacology Pub Date : 2004-11-01
Jerzy Kossakowski, Aldona Raszkiewicz, Ryszard Bugno, Andrzej J Bojarski
{"title":"Introduction of a new complex imide system into the structure of LCAPs. The synthesis and a 5-HT1A, 5-HT2A and D2 receptor binding study.","authors":"Jerzy Kossakowski,&nbsp;Aldona Raszkiewicz,&nbsp;Ryszard Bugno,&nbsp;Andrzej J Bojarski","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A series of 17 long-chain arylpiperazines containing bulky, complex imide systems (5,8-dimethyl-3b,9-epoxy-(3a,4,5,6,7,8,9,9a)-octahydro-1H-benzo[e]isoindole-1,3(2H)-dione or 4,9-diphenyl-4,9-epoxy-3a,4,9,9a-tetra-hydro-1H-benzo[f]isoindole-1,3(2H)-dione) was synthesized and evaluated for their affinity for serotonin 5-HT1A, 5-HT2A and dopamine D2 receptors. Most of the new compounds showed moderate activity at 5-HT1A binding sites (Ki = 100-492 nM), and two derivatives were found to have marked affinity for the 5-HT2A receptor subtype. None of the tested compounds displayed appreciable binding to dopamine D2 receptors Structure-activity relationships were discussed in respect to an arylpiperazine fragment, whereas the comparison of different imide terminals enabled determination of the size of a hydrophobic pocket (approximately 300 A3) within the 5-HT1A receptor.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"843-8"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24916280","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
Effect of metyrapone supplementation on imipramine therapy in patients with treatment-resistant unipolar depression. 补充美拉酮对难治性单极抑郁症患者丙咪嗪治疗的影响。
Polish journal of pharmacology Pub Date : 2004-11-01
Zofia Rogóz, Grazyna Skuza, Jacek Wójcikowski, Władysława A Daniel, Andrzej Wróbel, Dominika Dudek, Andrzej Zieba
{"title":"Effect of metyrapone supplementation on imipramine therapy in patients with treatment-resistant unipolar depression.","authors":"Zofia Rogóz,&nbsp;Grazyna Skuza,&nbsp;Jacek Wójcikowski,&nbsp;Władysława A Daniel,&nbsp;Andrzej Wróbel,&nbsp;Dominika Dudek,&nbsp;Andrzej Zieba","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The paper describes the effect of metyrapone supplementation on imipramine therapy in patients (with treatment-resistant unipolar depression) who fulfilled DSM IV criteria for major depression. Nine 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 imipramine twice daily (100 mg/day) for 6 weeks, and then metyrapone was introduced (twice daily, 500 mg/day), and administered jointly with imipramine for further 6 weeks. Hamilton Depression Rating Scale (HDRS) and Beck Depression Inventory (BDI) were used to assess efficacy of antidepressant therapy. Imipramine changed neither HDRS nor BDI score after 6 weeks of treatment when compared with baseline (before treatment). Metyrapone supplementation significantly reduced both HDRS and BDI scores after 6-week supplementation. Moreover, pharmacokinetic data indicate that metyrapone did not influence significantly the plasma concentration of imipramine and its metabolite, desipramine in the patients during joint treatment with metyrapone and imipramine, what suggests the lack of pharmacokinetic interaction. This preliminary study is the first demonstration of the benefit of metyrapone supplementation in imipramine therapy of treatment-resistant unipolar depression and suggests that a change in the level of neurotransmitters, hormones and immunological parameters, which are disturbed in depression, may contribute to the mechanism of the action of this drug.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"849-55"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24916281","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
Brain dopamine receptors--research perspectives and potential sites of regulation. 脑多巴胺受体——研究视角和潜在调控位点。
Polish journal of pharmacology Pub Date : 2004-11-01
Marta Dziedzicka-Wasylewska
{"title":"Brain dopamine receptors--research perspectives and potential sites of regulation.","authors":"Marta Dziedzicka-Wasylewska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Dopamine mediates its biological actions via at least five distinct G protein-coupled receptors. Recently, significant progress has been made in the understanding of the molecular and cellular consequences of activation of the different dopamine receptors. Not only their anatomical localization has been revisited, what implicates new insights into well known D1/D2 receptor synergism, but also evidence has been provided that dopamine receptors can physically interact with each other as well as with other neurotransmitter receptors. Dopamine receptors are subject to phosphorylation by G protein-coupled receptor kinases, the specificity of which has started to be revealed. Some progress has been made in elucidating the functional significance of polymorphisms observed in genes encoding dopamine receptor. All these new findings need to be appreciated by the psychopharmacologists in order to better understand the behavioral consequences of activation of dopamine receptors.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"659-71"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25084142","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
Involvement of nitricoxidergic system in the hypnotic effects of benzodiazepines in mice. 氮氧化能系统参与苯二氮卓类药物对小鼠的催眠作用。
Polish journal of pharmacology Pub Date : 2004-11-01
Sylwia Talarek, Sylwia Fidecka
{"title":"Involvement of nitricoxidergic system in the hypnotic effects of benzodiazepines in mice.","authors":"Sylwia Talarek,&nbsp;Sylwia Fidecka","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The influence of nitric oxide (NO) on hypnotic activity of diazepam, chlordiazepoxide and clonazepam was studied in mice. Administration of both non-selective NO synthase inhibitors: N(G)-nitro-L-arginine methyl ester (L-NAME), N(G)-nitro-L-arginine (L-NOARG) and selective NO synthase inhibitor 7-nitroindazole (7-NI) resulted in significant increase in the duration of diazepam-, chlordiazepoxide- and clonazepam-induced sleep. The effects of co-administration of the examined inhibitors with benzodiazepines were not changed by L-arginine, a substrate for NO formation. Administration of L-arginine alone had no effect on the duration of sleep induced by benzodiazepines. Methylene blue, the guanyl cyclase inhibitor, was able to increase the duration of benzodiazepine-induced sleep. These findings suggest that the cGMP/NO system may participate in hypnotic effects of benzodiazepines.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"719-26"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25084667","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
Potential role of the brain dopaminergic system in the regulation of cytochrome P-450 expression. 脑多巴胺能系统在细胞色素P-450表达调控中的潜在作用。
Polish journal of pharmacology Pub Date : 2004-11-01
Jacek Wójcikowski
{"title":"Potential role of the brain dopaminergic system in the regulation of cytochrome P-450 expression.","authors":"Jacek Wójcikowski","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Although there are no literature data, which would clearly describe the role of catecholaminergic systems (including dopaminergic system) in the expression of the liver cytochrome P-450, there are well documented reports on physiological regulation of cytochrome P-450 by endogenous hormones (glucocorticoids, sex hormones, thyroid hormones, growth hormone, insulin) and by the immune system (cytokines), and all these factors remain under central nervous system control. Therefore, one can expect that dysfunction of catecholaminergic systems may lead to significant changes in activities of particular cytochrome P-450 isoenzymes by altering levels of endogenous hormones. The mechanism underlying dopamine-induced regulation of the liver cytochrome P-450 expression seems not to be direct, but rather mediated by pituitary hormones and cytokines.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"701-8"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25084666","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
Neurogenesis in the adult brain. 成人大脑中的神经发生。
Polish journal of pharmacology Pub Date : 2004-11-01
Marzena Maćkowiak, Agnieszka Chocyk, Katarzyna Markowicz-Kula, Krzysztof Wedzony
{"title":"Neurogenesis in the adult brain.","authors":"Marzena Maćkowiak,&nbsp;Agnieszka Chocyk,&nbsp;Katarzyna Markowicz-Kula,&nbsp;Krzysztof Wedzony","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Neurogenesis is a process that involves cell proliferation, migration and differentiation. Adult neurogenesis has been discovered by Altman in the mid 1960s. It is known now that neurogenesis occurs in two main neurogenic areas of the adult mammalian brain: the olfactory bulb and the hippocampal dentate gyrus, although other brain regions, such as cortex or substantia nigra cannot be excluded. The rate of neurogenesis can be regulated in a positive and negative manner by several factors like, age, growth factors, hormones, environmental or pharmacological stimuli. Functional significance of adult neurogenesis is still under investigation, however, several evidences suggest involvement of newly generated neurons in cognitive processes. There are also several findings indicating that the impairment of adult neurogenesis may be involved in the pathophysiology of some brain diseases, like depression, epilepsy, ischemia or neurodegenerative disorders. It appears that alterations in the rate of neurogenesis may have important functional and therapeutic implications.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"673-87"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25084143","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
MPEP, mGlu5 receptor antagonist, regulates NPYmRNA expression in hippocampal and amygdalar neurons. MPEP, mGlu5受体拮抗剂，调节海马和杏仁核神经元中NPYmRNA的表达。
Polish journal of pharmacology Pub Date : 2004-11-01
Maria Smiałowska, Joanna M Wierońska, Piotr Brański, Ewa Obuchowicz, Andrzej Pilc
{"title":"MPEP, mGlu5 receptor antagonist, regulates NPYmRNA expression in hippocampal and amygdalar neurons.","authors":"Maria Smiałowska,&nbsp;Joanna M Wierońska,&nbsp;Piotr Brański,&nbsp;Ewa Obuchowicz,&nbsp;Andrzej Pilc","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Our earlier studies showed that the metabotropic glutamate receptor 5 (mGluR5) antagonist, MPEP, could regulate neuropeptide Y (NPY) neurons in the amygdala, influencing both peptide expression and its antianxiety effects. Two brain structures are particularly engaged in a regulation of anxiety, namely the amygdala and also the hippocampus. They both belong to the limbic system and contain NPY neurons and mGlu5 receptors. Therefore, in the present study, we examined the effect of MPEP on NPY and NPYmRNA expression in the amygdala and the hippocampus of the rat brain. NPY expression was studied by immunohistochemical method, and radioimmunoassay, and the NPY synthesis was examined using NPYmRNA in situ hybridization. Immunohistochemical localization of mGluR5 was also carried out. It was found that MPEP given 3 times every 8 h potently decreased NPYmRNA expression 30 min after the last dose in both those structures (to 8-20% of the control level). After single MPEP treatment, we did not observe any changes in NPYmRNA level in the hippocampus, and its decrease in the amygdala 6 h after MPEP administration. The obtained results suggest a positive regulatory control of NPY synthesis by mGlu5 receptors in hippocampal and amygdalar neurons.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"709-18"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25084145","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
Synthesis and cardiovascular activity of new 8-alkylamino-1,3-dimethyl-7-(2-hydroxy-3- piperazinopropyl)-3,7-dihydro-1H-purine-2,6-diones. 新型8-烷基氨基-1,3-二甲基-7-(2-羟基-3-哌嗪丙基)-3,7-二氢- 1h -嘌呤-2,6-二酮的合成及心血管活性
Polish journal of pharmacology Pub Date : 2004-11-01
Grazyna Chłoń-Rzepa, Maciej Pawłowski, Małgorzata Zygmunt, Barbara Filipek, Dorata Maciag
{"title":"Synthesis and cardiovascular activity of new 8-alkylamino-1,3-dimethyl-7-(2-hydroxy-3- piperazinopropyl)-3,7-dihydro-1H-purine-2,6-diones.","authors":"Grazyna Chłoń-Rzepa,&nbsp;Maciej Pawłowski,&nbsp;Małgorzata Zygmunt,&nbsp;Barbara Filipek,&nbsp;Dorata Maciag","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>7-{2-Hydroxy-3-[4-(2-phenoxyethyl)-piperazinyl-1-yl]-propyl}-1,3-di-methyl-3,7-dihydro-1H-purine-2,6-dione dihydrochloride (2), and several of its 8-alkylamino substituted derivatives (11-17) were synthesized and tested for electrocardiographic, antiarrhythmic and hypotensive activity. Also their alpha(1)- and alpha(2)-adrenoreceptor affinities were determined. It was found that compound 2, and its analogue 15 with 8-(2-morpholin-4-yl-ethylamino) substituent displayed a strong prophylactic antiarrhythmic activity in experimentally induced arrhythmia (LD50/ED50 = 54.9 and 55.0, respectively). The hypotensive activity was observed for 8-benzylamino (11) or 8-(pyridin-2-yl-methylamino) (12) analogues. All the new derivatives (11-17) and 2 showed a weak affinity for alpha1-(Ki = 0.225-1.400 microM) and alpha2-(Ki = 0.152-4.299 microM) receptors.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"755-66"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"25084671","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
Influence of beta-adrenergic antagonists on tear secretion in children. 肾上腺素能拮抗剂对儿童泪液分泌的影响。
Polish journal of pharmacology Pub Date : 2004-11-01
Elzbieta Samochowiec-Donocik, Bronisława Koraszewska-Matuszewska
{"title":"Influence of beta-adrenergic antagonists on tear secretion in children.","authors":"Elzbieta Samochowiec-Donocik,&nbsp;Bronisława Koraszewska-Matuszewska","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The aim of the study was to compare the results of tear film volume, conjunctival and corneal state of children eyes both treated with beta-blocker and healthy ones. We have examined 40 eyes of 20 children at the age from 7 to 17 years. Group I - 20 glaucomatous eyes treated with 0.5% timolol twice daily during at least 12 months. Group II - 20 eyes of control age-matched group. Schirmer I test without anesthesia and lissamine green staining was performed to evaluate conjunctival and corneal surface. The values of Schirmer I test were: group I from 12 to 24 mm, the mean 17.06 +/- 1.78 mm and group II from 16 to 35 mm, the mean 29.3 +/- 2.67, p = 0.000004. Keratoepitheliopathy was observed in 4 eyes (20%) of group I and was rated as 3rd and 6th degree of Franck classification. In the group II, there were only single staining points classified as 1st degree noticed in 2 eyes (10%), p = 0.37. The long-term treatment with timolol causes a decrease in tear secretion in children, which can further generate keratoepiteliopathy. Therefore, we suggest application of the artificial tears in these patients.</p>","PeriodicalId":20292,"journal":{"name":"Polish journal of pharmacology","volume":"56 6","pages":"871-3"},"PeriodicalIF":0.0,"publicationDate":"2004-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"24916285","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
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