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61.
Selective blockade of muscarinic M2 receptors in vivo by the new antagonist tripitramine 总被引:1,自引:1,他引:0
Piero Angeli Franco Cantalamessa Ugo Gulini Carlo Melchiorre 《Naunyn-Schmiedeberg's archives of pharmacology》1995,352(3):304-307
The antimuscarinic effects of tripitramine (1, 1, 24--tris [[5, 11-dihydro-6-oxo-6H-pyrido [2, 3-b][1, 4]-benzodiazepin-11-yl)(carbonyl] methyl]-8, 17-dimethyl-1, 8, 17, 24-tetraazatetracosane tetraoxalate), a member of a series of polymethylene tetraamines with in vitro cardioselectivity, were assessed in two in vivo preparations: anaesthetized and pithed rats. The well-known M2 selective antagonist methoctramine was used in a comparative study. Tripitramine (0.0202 mol/kg i.v.) proved to be a potent antagonist at cardiac M2 receptors that mediate the decrease in heart rate in the pithed rat; the same dose of this antagonist in the anaesthetized rat did not significantly affect the depressor action of methacholine mediated by vascular M3 receptors. In the pithed rat, this dose did not affect the ganglionic M1 receptor-mediated tachycardia and pressor response to muscarme or McN-A-343. These in vivo data are consistent with the in vitro findings and confirm that tripitramine is a more potent and selective muscarinic M2 receptor antagonist than methoctramine. 相似文献
62.
63.
Tight junction proteins claudin-3 and claudin-4 are frequently overexpressed in ovarian cancer but not in ovarian cystadenomas. 总被引:18,自引:0,他引:18
64.
Value of P-glycoprotein and clinicopathologic factors as the basis for new treatment strategies in high-grade osteosarcoma of the extremities. 总被引:8,自引:0,他引:8
Massimo Serra Katia Scotlandi Gemma Reverter-Branchat Stefano Ferrari Maria C Manara Stefania Benini Marina Incaprera Franco Bertoni Mario Mercuri Antonio Briccoli Gaetano Bacci Piero Picci 《Journal of clinical oncology》2003,21(3):536-542
PURPOSE: To evaluate the prognostic value of P-glycoprotein and clinicopathologic parameters in a large series of high-grade osteosarcoma (OS) patients treated at the Rizzoli Institute. PATIENTS AND METHODS: With the use of immunohistochemistry, P-glycoprotein was assessed in 149 patients with primary, nonmetastatic, high-grade OS who were homogeneously treated with chemotherapy protocols based on doxorubicin, high-dose methotrexate, and cisplatin and the addition of ifosfamide in the postoperative phase. RESULTS: P-glycoprotein positivity was found in 47 of 149 cases (32%) and was significantly associated with a higher incidence of relapse and a worse outcome, as was age younger than 12 years and tumor volume greater then 150 mL at diagnosis. Multivariate analysis further confirmed the prognostic value of these parameters, which all were independent adverse prognostic factors. Event-free survival and proportional hazards regression analyses confirmed that overexpression of P-glycoprotein at clinical onset is the most important adverse prognostic factor for high-grade OS patients treated with these chemotherapy protocols. CONCLUSION: Increased P-glycoprotein levels, together with tumor volume and age, should be taken into consideration to identify, at time of diagnosis, subgroups of OS patients with a higher risk of recurrence. This subgroup identification will constitute the basis for drawing individualized treatment protocols on the basis of risk evaluation, with the aim of using more aggressive chemotherapy, or combination chemotherapy with other adjuvants, only in those patients for which more aggressive regimens are strictly necessary and warranted. 相似文献
65.
Gabriella Marucci Angeli Piero Livio Brasili Michela Buccioni Dario Giardinà Ugo Gulini Alessandro Piergentili Gianni Sagratini 《Medicinal chemistry research》2005,14(5):274-296
Geometric cis, trans isomers, derivatives of 2-substituted-1,3-dioxanes were designed and studied as antimuscarinic agents. The synthesized compounds
were evaluated as perchlorides and methiodides by functional tests with rabbit vas deferens (putative M1), guinea-pig heart (M2) and guinea-pig ileum (M3). The effect of the replacement of a trimethylammonium group with a dimethysulfonium in the two rings was also evaluated.
Pharmacological results indicate that the 1,3-dioxane nucleus shows the highest stereoselective values on the studied receptors. 相似文献
66.
Spontaneous esophageal perforation (Boerhaave's syndrome) remains a difficult diagnostic and management problem with controversial recommendations regarding its treatment. The clinical manifestations of the disease are variable, and may be misleading, thus delaying accurate recognition. On the other hand, in view of the rapid onset of severe complications, particularly mediastinitis, a prompt diagnosis is essential to a better prognosis, successful operative outcome and potential survival. A case of spontaneous perforation of the thoracic esophagus penetrating the left pleural space treated within 4 hours from admission to the Emergency Room, with minimal surgical intervention is presented. Despite negative chest X-ray, a thoracic TC showed a small right sided effusion with left sided hydropneumothorax, and the definitive diagnosis was obtained by contrast study with a water soluble medium which showed the leak communicating freely with the left pleural space. The patient underwent repair by thoracic approach, the rupture was closed with a primary suture without flap reinforcement and the pleural space drained with the placement of single chest thoracostomy tube. The recovery was uneventful. The analysis of this case report and of the appropriate literature reveals that a poor prognosis is correlated with the time elapsed between the perforation and treatment. In conclusion the importance of an early aggressive surgical treatment for the Boerhaave's syndrome is emphasized, because any perforation treated more than 24 hours after the onset of symptoms, irrespective of the procedure used, is associated with a significantly higher morbility and mortality. 相似文献
67.
Gian Piero Siliquini MD Valentina Elisabetta Bounous MD PhD Lorenzo Novara MD Margherita Giorgi MD Fabrizio Bert MD Nicoletta Biglia MD PhD 《The breast journal》2021,27(5):448-455
Adjuvant chemotherapy and endocrine therapy can induce early iatrogenic menopause or worsen pre-existing menopausal symptoms in breast cancer survivors (BCS). The second most frequent menopausal symptom after hot flushes is the genitourinary syndrome (GSM). Since hormone replacement therapy is contraindicated in BCS, vaginal laser might represent a new nonhormonal option for GSM. This study aims at evaluating the effectiveness of the fractional CO₂ vaginal laser for GSM in BCS compared with healthy women. This is a retrospective study on 135 postmenopausal women (45 BCS and 90 healthy women) who underwent fractional CO2 laser for GSM. Objective (VHI and VVHI) and subjective outcomes (VAS for dyspareunia and vaginal dryness and a pain questionnaire) were evaluated at baseline visit and at every follow-up visit. Subjective and objective parameters improved significantly in both groups after laser therapy. The improvement was progressive and long-lasting up to 12 months after the end of the treatment. No severe adverse events were observed during the treatment. Fractional CO₂ vaginal laser induces a significant and long-lasting improvement on GSM symptoms in BCS. However, this improvement is slower than in healthy women undergoing the same treatment. Laser therapy turns out to be safe and well-tolerated. 相似文献
68.
Mauro Giammarino Piero Quatto Stefania Squadrone Maria Cesarina Abete 《Bulletin of environmental contamination and toxicology》2014,93(4):410-416
This study aims to examine the possible presence of lead and cadmium in the liver and kidneys of hooded crows (Corvus cornix). Liver and kidneys of hooded crow carcasses were collected in Province of Cuneo (Piedmont, Italy) in order to detect lead and cadmium content. Significant differences were found in lead and cadmium levels between areas of intensive cultivation versus areas where meadows are prevalent. Moreover, age greatly influenced the burden of heavy metals, while sex did not seem to affect the level of contamination. The source of contamination may be phosphate fertilizers used for intensive cultivation in the study area. 相似文献
69.
Eduardo Alexandre Loth Samia Khalil Biazim José Henrique Fermino Ferreira dos Santos Rosana Puccia Rosimeire Costa Brancalh?o Lucinéia de Fátima Chasco Rinaldo Ferreira Gandra Rita de Cássia Garcia Sim?o Marcello Fabiano de Franco 《Revista do Instituto de Medicina Tropical de S?o Paulo》2014,56(3):259-264
Paracoccidioidomycosis (PCM) is caused by the dimorphic fungus
Paracoccidioides brasiliensis (Pb) and corresponds to prevalent
systemic mycosis in Latin America. The aim of the present work was to evaluate the
dose response effect of the fungal yeast phase for the standardization of an
experimental model of septic arthritis. The experiments were performed with groups of
14 rats that received doses of 103, 104 or 105
P. brasiliensis (Pb18) cells. The fungi were injected in 50 µL of
phosphate-buffered saline (PBS) directly into the knee joints of the animals. The
following parameters were analyzed in this work: the formation of swelling in knees
infused with yeast cells and the radiological and anatomopathological alterations,
besides antibody titer by ELISA. After 15 days of infection, signs of inflammation
were evident. At 45 days, some features of damage and necrosis were observed in the
articular cartilage. The systemic dissemination of the fungus was observed in 11% of
the inoculated animals, and it was concluded that the experimental model is able to
mimic articular PCM in humans and that the dose of 105 yeast cells can be
used as standard in this model. 相似文献
70.