Syntheses of Novel Pyridazinomorphinans by Inverse Electron Demand Cycloaddition and their Binding to μ and κ Receptors     

Thilo Klindert  Isabel Stroetmann  Gunther Seitz  Georg Hfner  Klaus Th. Wanner  Gerlinde Frenzen  Brigitta Eckhoff 《Archiv der Pharmazie》1997,330(6):163-168

A number of novel pyridazinomorphinans have been synthesized by the inverse electron demand Diels-Alder reaction of various 3,6-disubstituted 1,2,4,5-tetrazines with enamines derived from dihydrocodeinone and with codeinone. Reduction of some of the pyridazinomorphinans did not furnish the expected pyrroloepoxymorphinans; in all cases investigated reductive cleavage of the epoxybridge was observed to yield dihydropyridazino- or pyrrolomorphinans. The structures of all new compounds were assigned by the spectral data, that of the cycloadduct of codeinone was additionally verified by X-ray crystallography. Compounds 5a, 8, 11a , and 16 have been evaluated for their affinity at μ and κ opioid receptors in radioligand binding assays. Their ability to inhibit [³H]DAMGO binding at μ and [³H]U 69.593 binding at κ receptors, respectively as compared to codeine has been found to be lower.  相似文献   

Comparative effects of enoximone and theophylline on plasma catecholamines and haemodynamics in cardiosurgical patients     

J. Boldt  H. A. Adams  B. Zickmann  D. Kling  G. Hempelmann 《European journal of clinical pharmacology》1990,38(5):431-436

Summary The release of endogenous catecholamines in aorto-coronary bypass graft patients receiving either 0.5 mg/kg enoximone (n=10), 4.0 mg/kg theophylline (n=10) or saline solution (control,n=10) has been studied, as well as certain haemodynamic parameters. Adrenaline (A) and noradrenaline (NA) concentrations were not significantly changed by the administration of enoximone. Theophylline caused a small increase in NA (+ 40% in the 1st min) and a marked increase in A (approximately + 7000% in the 1st min), which still remained elevated at the end of the investigation period (+ 220% in the 30th min). The major haemodynamic effects of enoximone were a significant increase in cardiac index (CI; + 35%) and a decrease in pulmonary capillary wedge pressure (PCWP; −27%), pulmonary artery pressure (PAP; −21%), RVEDV and RVESV, while the heart rate (HR) remained almost unchanged. The dominant haemodynamic effects of theophylline were an increase in HR (+ 26%; arrhythmia in 3 patients), PAP (+ 22%), and RVEDV (+ 19%), while REVESV (+ 26%), MAP (−16%), CI (−14%), and RVEF (−15%) fell significantly. It is concluded that the haemodynamic actions of enoximone are not mediated by catecholamine release, whereas the adverse cardiovascular effects of theophylline might partly be explained by the significant increase in plasma adrenaline.  相似文献   

Substance P and human nasal mucociliary activity   总被引：2，自引：0，他引：2  

G. Karlsson  U. Pipkorn  L. Andreasson 《European journal of clinical pharmacology》1986,30(3):355-357

Summary Substance P (SP), a potent inflammatory agent, has been found in sensory nerve fibres in the nasal mucosa in several experimental animals as well as in man. It may participate in the inflammatory response as part of the mucosal defence against foreign materials. In experimental animals SP has been found to increase mucociliary in airway mucosa. The present study was performed in order to find out the relationship between topically applied SP and nasal mucociliary function in humans. Thirteen healthy volunteers were challenged with 65 µg SP or placebo in a randomized cross over fashion and mucociliary transport time was determined each time using the saccharine dye test. The dose of SP was chosen after an open dose-response study. No statistically significant change in the mucociliary transport time was found after challenge with SP as compared to placebo. The possible reasons for this are discussed.  相似文献   

Propriospinal myoclonus after treatment with ciprofloxacin.     

Bart Post  Johannes H T M Koelman  Marina A J Tijssen 《Movement disorders》2004,19(5):595-597

The clinical and electrophysiological features of a truncal myoclonus in a 55-year-old man are described. The electromyographic characteristics point toward propriospinal myoclonus. It is suggested that a myoclonic generator was released after use of ciprofloxacin, by antagonising the gamma-aminobutyric acid metabolism.  相似文献   

Maculopapular eruption with enlarged macrophages in eight patients receiving G-CSF or GM-CSF     

S Álvarez-Ruiz†  PF Peñas†  J Fernández-Herrera†  J Sánchez-Pérez†  J Fraga‡  A García-Díez† 《Journal of the European Academy of Dermatology and Venereology》2004,18(3):310-313

In the last years, granulocyte and granulocyte-macrophage colony-stimulating factors (G-CSF and GM-CSF) are being increasingly used and several cutaneous eruptions have been reported in relation to these treatments. In 1991 Horn et al. described three patients with maculopapular eruption that paralleled the time of infusion of GM-CSF. Two of the cases showed an increase in the number and size of macrophages in the biopsy specimen. Since then, several cases have been reported showing this histopathological alteration that has been considered characteristic of reaction to G-CSF or GM-CSF. Although maculopapular eruption with enlarged macrophages can appear after chemotherapy treatment, we have found that the presentation of this eruption after the beginning of cytokine treatment is suggestive of the involvement of G-CSF and GM-CSF in the eruption. We described eight cases of patients treated with G-CSF or GM-CSF that developed maculopapular eruptions with enlarged macrophages.  相似文献   

Cyclic hormonal replacement therapy after the menopause: Transdermal versus oral treatment   总被引：2，自引：0，他引：2  

M. Cortellaro  T. Nencioni  C. Boschetti  S. Ortolani  F. Buzzi  B. Francucci  M. P. Caraceni  P. Abelli  F. Polvani  C. Zanussi 《European journal of clinical pharmacology》1991,41(6):555-559

Summary In an open, randomized, comparative, between-patient trial, 45 postmenopausal women were treated for 4 months with cyclical transdermal oestradiol 0.05 mg per day or oral conjugated equine oestrogens 0.625 mg per day, in both cases, plus, medroxyprogesterone acetate 10 mg per day on the last 8 days of each cycle. Similar relief from postmenopausal symptoms was obtained with both treatments. Post-treatment histological evaluation of the endometrium did not reveal neoplastic or hyperplastic change in any patient.Early follicular-phase plasma oestradiol levels were observed only after transdermal oestradiol. There was a significant reduction in serum total cholesterol and LDL cholesterol in both treatment groups, with no difference between treatments, whereas serum triglyceride levels were decreased only by transdermal oestradiol. Plasma calcium and phosphorus fell significantly and serum intact parathyroid hormone rose significantly, with no difference between the therapies. No significant changes were observed in clotting factors.Transdermal oestradiol appears to be an effective and safe hormonal replacement therapy, and this route of administration may be responsible for the more useful action of the drug on serum lipids and plasma oestradiol levels.  相似文献   

Dihematoporphyrin ether-induced photosensitivity in laryngeal papilloma patients   总被引：2，自引：0，他引：2  

V M Mullooly  A L Abramson  M J Shikowitz 《Lasers in surgery and medicine》1990,10(4):349-356

Twenty-six patients with recurrent laryngeal papillomatosis received 2.5 mg/kg of Dihematoporphyrin Ether (DHE) intravenously prior to photodynamic therapy. All patients experienced some degree of photosensitivity, the only known side effect of DHE. Reported reactions included mild erythema and inflammation (88%), swelling (58%), blistering (23%), ocular discomfort (61.5%), pruritus (38%), and skin hyperpigmentation (46%). Length of sensitivity ranged from 4-17 weeks, with an average duration of 9 weeks. No long-term debilitating sequelae were noted. Degree of skin reaction mainly depended on how compliant the patient was in following precaution instructions. Although restrictive precautions were often difficult to strictly adhere to, most patients felt the potential benefits of the therapy far outweighed any inconvenience.  相似文献   

Microscopic haematuria as a relative contraindication for tranexamic acid     

Marc  Schultz Hans  van der Lelie 《British journal of haematology》1995,89(3):663-664

Tranexamic acid has been advocated for patients with severe bleeding tendency due to thrombocytopenia not responding to platelet transfusions. Macroscopic haematuria is a well-known contraindication for its use in such patients. We present three clinical cases with microscopic haematuria, in whom tranexamic acid caused problems of clot formation in the urinary tract, indicating that microscopic haematuria should also be considered as a contraindication for tranexamic acid.  相似文献   

Supercritical fluids in medical radioisotope processing and chemistry,Part II: Applications – real and demonstrated     

《Journal of labelled compounds & radiopharmaceuticals》2003,46(10):923-943

In Part I of this review series, an overview was presented on what the basic properties of supercritical fluids are and how they can, and are being used in many of today's industries as solvents for extraction, chromatography and reaction. A good part of this overview detailed the kinds of equipment needed, and techniques on how to use them for optimal performance. Part II of this series will delve into specific applications of supercritical fluid technology as it relates to aspects of medical isotope processing. The reader will note that very few applications of this technology to Nuclear Medicine have been published. Many potential applications cited within the context of this review derive from preliminary studies carried out in the author's laboratory. These examples are presented to spark interest in future developments of this nature. Copyright © 2003 John Wiley & Sons, Ltd.  相似文献   

Patch test reading at day 2 will not suffice     

Anil  Sony 《Contact dermatitis》1997,37(4):188-189

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