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排序方式: 共有10000条查询结果,搜索用时 15 毫秒
31.
Wassim Daher Lydie Pelinski Sylvie Klieber Freddy Sadoun Viviane Meunier Martine Bourrié Christophe Biot Fran?ois Guillou Gérard Fabre Jacques Brocard Laurent Fraisse Jean-Pierre Maffrand Jamal Khalife Daniel Dive 《Drug metabolism and disposition》2006,34(4):667-682
Ferroquine (SSR97193) has been shown to be a promising antimalarial, both on laboratory clones and on field isolates. So far, no resistance was documented in Plasmodium falciparum. In the present work, the metabolic pathway of ferroquine, based on experiments using animal and human hepatic models, is proposed. Ferroquine is metabolized mainly via an oxidative pathway into the major metabolite mono-N-demethyl ferroquine and then into di-N,N-demethyl ferroquine. Some other minor metabolic pathways were also identified. Cytochrome P450 isoforms 2C9, 2C19, and 3A4 and, possibly in some patients, isoform 2D6, are mainly involved in ferroquine oxidation. The metabolites were synthesized and tested against the 3D7 (chloroquine-sensitive) and W2 (chloroquine-resistant) P. falciparum strains. According to the results, the activity of the two main metabolites decreased compared with that of ferroquine; however, the activity of the mono-N-demethyl derivative is significantly higher than that of chloroquine on both strains, and the di-N-demethyl derivative remains more active than chloroquine on the chloroquine-resistant strain. These results further support the potential use of ferroquine against human malaria. 相似文献
32.
Contractile actions of thrombin receptor-derived polypeptides in human umbilical and placental vasculature: evidence for distinct receptor systems. 总被引:1,自引:1,他引:0 下载免费PDF全文
J. Tay-Uyboco M. C. Poon S. Ahmad M. D. Hollenberg 《British journal of pharmacology》1995,115(4):569-578
1. We studied the structure-activity profiles of four thrombin receptor-derived polypeptides (TRPs) (P5, SFLLR; P5-NH2, SFLLR-NH2; P7, SFLLRNP; P7-NH2, SFLLRN) in contractile human placental artery (PA), umbilical artery (UA) and umbilical vein (UV) preparations and in a human platelet aggregation assay. 2. The contractile actions of the TRPs in the two arterial preparations were endothelium-independent, whereas in the UV tissue a contractile response was observed only in an endothelium-denuded preparation; no endothelium-mediated relaxation responses were observed in any of the vascular preparations. 3. In the three vascular preparations, the contractile responses required extracellular calcium and were attenuated by the tyrosine kinase inhibitor, genistein. 4. The relative contractile orders of potencies of the TRPs in the three vascular preparations were distinct from each other (PA: P7-NH2 > P7 > P5-NH2 > P5; UA: P7-NH2 > or = P5-NH2 approximately = P7 > > P5; UV: P5-NH2 > > P7-NH2 = P7 > > P5) and these were in turn distinct from the potency order observed in the platelet aggregation assay (P5-NH2 > or = P7-NH2 > P7 > > P5). 5. Despite the markedly dissimilar TRP potency orders in the placental artery and umbilical vein preparations, the cDNA sequences for the thrombin receptor obtained by polymerase chain reaction cloning of cDNA from the two tissue sources were identical. 6. We conclude that the four tissues studied possess functionally distinct thrombin receptor systems that interact in a distinct way with agonist peptides. In view of the identity of the thrombin receptor cDNA in the two tissues displaying the most dissimilar structure-activity profiles, we suggest that in different tissues, differences in post-translational receptor processing or differences in receptor-effector coupling interactions may result in unique thrombin receptor systems that can display distinct structure-activity profiles. 相似文献
33.
Patients with occlusive arterial diseases, tumors invading the vascular structures of the skull base or giant aneurysms may benefit from an EICB. Most of the time this can be achieved using a scalp artery. But in cases of a thrombotic ECA, excessively short or thin scalp branches or destruction of those by prior cranial surgery, an interposed venous graft is needed. In the author's series, which consists of 16 patients, the bypass was performed for ICA occlusive diseases in 5, before complete removal of cavernous sinus tumours in 4 and prior to cervical internal carotid ligation for giant aneurysms in 7. The grafts were always harvested from the internal saphenous vein. The proximal site of implantation was CCA (2 cases), ECA (6 cases), ICA (1 case), superior thyroid A (2 cases)--i.e. 11 long grafts--and the trunk of the occipital A--i.e. short grafts in 5 cases. In this series, there was no mortality and no morbidity related to revascularization. The early patency rate, checked with arteriography, was 62.5% (10 cases) and the late one 56.2% (9 cases). Causes of failure, partially related to technical difficulties in 2 cases, were almost always due to an insufficient extra-intracranial pressure gradient (4 cases). Excepted in one case, there was no correlation between patency and the use or not of anti-aggregant and/or heparin. Literature data are summarized and discussed. They all confirm the importance--besides the absence of technical errors--of a sufficient extra-intracranial gradient for obtaining a good patency rate. 相似文献
34.
Andreas Granetzny Ashraf Hatem Alaa Shalaby Ahmad Boseila 《European journal of cardio-thoracic surgery》2005,27(3):361-366
OBJECTIVE: In a prospective study, the effect of thymectomy on the pulmonary status of 50 consecutive patients with myasthenia gravis was evaluated over a time range of 4 years in the Chest and Chest surgery departments in the Cairo University Clinics and Thoracic Surgery Department of the Evangelisches Krankenhaus Duisburg-Nord. METHODS: The patients were divided into two groups: Group I included 26 patients who underwent thymectomy through median sternotomy. The mean age of the patients in this group was 24.8+/-10.5 (5-41) years. They were 19 females and seven males. Thirteen of the patients were in Myasthenia Gravis Foundation of America (MGFA) class IIa, and 12 were in class IIb, and one was in class IIIa. Group II included 24 patients who underwent thymectomy through manubriotomy. The mean age of the patients in this group was 25.2+/-9.2 (12-41) years. They were 13 females and 11 males. Eight of the patients were in MGFA class 2a, 14 were in class IIb, and two were in class IIIa. RESULTS: When compared to group I in which postoperative ventilation was required in 15.4% of patients, postoperative ventilation was not necessary in patients of group II with a statistically significant difference (P=0.04). The mean duration of stay in the intensive care unit was 111.4h in group II, and 169.7h in group I (P=0.03). The peak inspiratory flow rate and the forced vital capacity were also statistically significantly better in group II. There was no mortality in both groups, and the morbidity was higher in the median sternotomy group. CONCLUSION: Thymectomy through a manubriotomy, which allows extensive removal of ectopic thymic tissue in addition to the thymus through a less invasive approach than a full median sternotomy, is associated with a significantly smoother postoperative course and less pulmonary complications, when compared with thymectomy through a full median sternotomy. 相似文献
35.
Ahmad Y. Sheikh MD ; Mark D. Rollins MD PhD ; Harriet W. Hopf MD ; Thomas K. Hunt MD 《Wound repair and regeneration》2005,13(3):303-308
There is a need for a noninvasive method that measures wound angiogenesis. Hyperoxia is known to increase the appearance of new blood vessels in wounds, yet no study has confirmed increases in wound bed perfusion with periodic hyperbaric oxygen (HBO) exposure. This study investigates whether laser Doppler imaging is able to detect and quantify the enhancement of wound angiogenesis that is known to occur with intermittent HBO treatments. Full-thickness dorsal dermal wounds were created on mice randomized to hyperoxic (n = 14) and control (n = 15) groups. Hyperbaric oxygen was administered twice daily for 90 minutes each at 2.1 atmospheres for 7 days. Wound bed perfusion was measured by laser Doppler imaging on days 0, 7, and 10 postwounding. Wound blood flow increased significantly over baseline on day 7 and 10 in the hyperoxic group, but only on day 10 in the control group. Comparison between groups showed a 20% statistically significant increase in wound perfusion in HBO-treated animals compared to control on day 10 (p = 0.05). Laser Doppler imaging was able to detect and quantify the increase in wound bed perfusion resulting from intermittent HBO treatments and shows promise as a noninvasive measure of angiogenesis and wound healing. 相似文献
36.
Ali S. Ziaee Nadia Khatibzadeh Alireza Rahimnia Ahmad S. Mousavi Shaban Mehrvarz 《European journal of orthopaedic surgery & traumatology : orthopedie traumatologie》2005,15(4):270-274
The aim of this study is to identify the effect of time and pressure of tourniquet in blood pressure and pulse rate immediately after the releasing of tourniquet in the upper and lower extremity of the orthopedic surgeries. This retrospective study examined 206 consecutive patients. Comparisons of the systolic and diastolic pressure and heart rate were made before the induction of anesthesia and tourniquet inflation, and immediately after the deflation. In general, there was no significant difference in hemodynamic changes between the upper- and lower-limb with regard to the type of anesthesia. There was no significant correlation between systolic blood pressure and tourniquet pressure, while by increasing the tourniquet time significantly, the systolic blood pressure decreases immediately after the deflation. Interestingly, the considerable increase in age paralleled with a significant decrease in the systolic blood pressure. The effect of tourniquet time is more than the age. There was no significant correlation between the tourniquet pressure and tourniquet time with diastolic blood pressure. Simply the increase in age significantly paralleled with the mild decrease in diastolic blood pressure Orthopedic surgeons are recommended not to rely on the benefits of tourniquet to raise blood pressure due to hypotensive conditions after the deflation especially in the old. 相似文献
37.
Omidvari Shapour MD Nezakatgoo Nosrat MD † Ahmadloo Niloofar MD Mohammadianpanah Mohammad MD Mosalaei Ahmad MD 《Dermatologic surgery》2005,31(5):499-501
BACKGROUND: Hemangioma is the most common tumor of infancy. Although it has a basically benign nature and usually spontaneously regresses, a small percentage (5%) have complications that need treatment. Many different therapeutic modalities can be used in this tumor. OBJECTIVE: To investigate the effect of a new method of treatment (intralesional bleomycin injection) in complicated hemangiomas. MATERIALS AND METHODS: In the Department of Radiation Oncology at Nemazee Hospital in Shiraz, Iran, from April 1992 to October 1998, 32 patients with complicated hemangioma were treated with four to six courses of direct injection of bleomycin into the lesion. RESULTS: After a minimum follow-up of 6 years, there was 70 to 100% regression in 18 patients, 50 to 70% in 7 cases, and less than 50% reduction in 7 patients. CONCLUSION: Intralesional injection of bleomycin is an easy, safe, and effective therapeutic modality in complicated cutaneous hemangiomas. 相似文献
38.
39.
M. Ahmad Agil S. Risco M. Mir M. C. Navarro M. A. Ocete J. Jimnez 《Phytotherapy research : PTR》1995,9(2):135-138
The dried (elaterium) or fresh juice from Ecballium elaterium fruit is used in the treatment of various inflammatory conditions in popular medicine. In this study the elaterium is examined for its analgesic and antipyretic effects in several animal models. The elaterium exhibits both analgesic and antipyretic activities. 相似文献
40.