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Combination of N-methyl-D-aspartate receptor antagonists and propofol for procedural sedation 认领 引用
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作者 Muhammad Shaheer Bin Faheem Syed Tawassul Hassan +6 位作者 Faheem Feroze Ayesha Khan Syeda Umbreen Munir Ali Khaliq Syeda Takreem Fatima Roni Mendonca Salim Surani 《World Journal of Clinical Cases》 2026年第8期24-43,共20页
BACKGROUND Propofol is widely considered for procedural sedation and analgesia across medical facilities.It is associated with dose-dependent hypotension,respiratory depression,and lack of analgesia.These limitations ... BACKGROUND Propofol is widely considered for procedural sedation and analgesia across medical facilities.It is associated with dose-dependent hypotension,respiratory depression,and lack of analgesia.These limitations can be managed by combining propofol with N-methyl-D-aspartate(NMDA)receptor antagonists(ketamine/esketamine);however,previous reviews have not fully synthesized the data on both agents.AIM To investigate the safety and efficacy of combining NMDA receptor antagonists(ketamine or esketamine)with propofol compared to propofol monotherapy for procedural sedation.METHODS Randomized controlled trials comparing NMDA antagonist-propofol combinations with propofol mo-notherapy were searched across PubMed,EMBASE,and ClinicalTrials.gov through June 2025.A random-effects model pooled risk ratios(RRs)and mean differences with 95%confidence intervals(CIs),and I2 statistics quantified heterogeneity,which was reduced through sensitivity,subgroup,and meta-regression analyses.RESULTS Nineteen randomized controlled trials(n=8400+)were included,from which 13 assessed ketamine-propofol,while 6 assessed esketamine-propofol.Combination therapy significantly reduced hypotension(RR=0.40;95%CI:0.26-0.60)and the need for respiratory interventions(RR=0.73;95%CI:0.58-0.93),whereas hallucinations were significantly more frequent in the intervention cohort(RR=2.24;95%CI:1.65-3.03).No significant differences were observed for desaturation,apnea,recovery time,systolic/diastolic blood pressure,mean arterial pressure,or heart rate.Patient satisfaction was comparable across groups.Sensitivity and subgroup analyses confirmed the strength of the key findings,and meta-regression revealed an increased risk of hypotension with higher propofol dosing,which was reduced with higher ketamine dosing.CONCLUSION NMDA antagonist-propofol regimen improves hemodynamic safety and reduces respiratory interventions in procedural sedation and analgesia compared to propofol,but is associated with a higher risk of hallucinations.These findings support the selective use of this approach,with dosing strategies justifying further modifications. 展开更多
关键词 N-methyl-D-aspartate receptor antagonists Ketamine Esketamine Propofol Procedural sedation
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Endothelin receptor antagonists for the treatment of diabetic nephropathy:A meta-analysis and systematic review 认领 引用 被引量：6
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作者 Li Zhang Shuai Xue +2 位作者 Jie Hou Guang Chen Zhong-Gao Xu 《World Journal of Diabetes》 SCIE 2020年第11期553-566,共14页
BACKGROUND Diabetic nephropathy(DN)is the main cause of chronic kidney disease and endstage renal disease worldwide.Although available clinical trials have shown that endothelin receptor(ER)antagonists may be a novel ... BACKGROUND Diabetic nephropathy(DN)is the main cause of chronic kidney disease and endstage renal disease worldwide.Although available clinical trials have shown that endothelin receptor(ER)antagonists may be a novel and beneficial drug for DN,no consistent conclusions regarding their sufficient effectiveness and safety for patients with DN have been presented.AIM To assess the effectiveness and safety of ER antagonists among patients with DN.METHODS The EMBASE,PubMed,MEDLINE,Cochrane,and ClinicalTrials.gov databases were searched without any language restrictions.Relative risks with 95%confidence intervals(CIs)for dichotomous data and mean differences or standardized mean difference with 95%CIs for continuous data were calculated using Review Manager 5.3 software.Publication bias was assessed using Egger’s test with Stata/SE software.RESULTS We enrolled seven studies with six data sets and 5271 participants.The ER antagonists group showed a significantly greater reduction in albuminuria and more patients with 40%reduction in urinary albumin-to-creatinine ratio than the control group(P<0.0001 and P=0.02,respectively).Subgroup analysis for reductions in estimated glomerular filtration rate(eGFR)showed that for the middle-dosage subgroup,the ER antagonists group exhibited lower eGFR reduction than the control group(P<0.00001;mean difference,0.7095%CI:0.66,0.74).Moreover,significant reductions in systolic and diastolic blood pressure were observed in the invention group.CONCLUSION ER blockades combined with angiotensin converting enzyme inhibitor/angiotensin II type 1 receptor blockers may be an effective treatment to lower blood pressure and reduce proteinuria in DN with declined eGFR.However,attention should be given to adverse events,including cardiac failure,anemia,and hypoglycemia,as well as serious adverse events. 展开更多
关键词 Endothelin receptor Endothelin receptor antagonists Endothelin receptor blockade Diabetic nephropathy Meta-analysis Systematic review
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Androgen deprivation therapy and side effects:are GnRH antagonists safer? 认领 引用 被引量：7
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作者 Stephen J Freedland Per-Anders Abrahamsson 《Asian Journal of Andrology》 SCIE CAS CSCD 2021年第1期3-10,共8页
Androgen deprivation therapy(ADT)with gonadotropin-releasing hormone(GnRH)agonists and antagonists is the mainstay of advanced prostate cancer treatment.Both drug classes decrease levels of luteinizing hormone and fol... Androgen deprivation therapy(ADT)with gonadotropin-releasing hormone(GnRH)agonists and antagonists is the mainstay of advanced prostate cancer treatment.Both drug classes decrease levels of luteinizing hormone and follicle-stimulating hormones(FSH),thereby lowering testosterone to castrate levels.This is associated with adverse events(AEs),including cardiovascular(CV)disorders,bone fractures,metabolic dysfunction,and impaired cognitive function.This literature review discusses these AEs,with a focus on CV and bone-related events.A hypothesis-generating meta-analysis of six clinical trials showed a potentially increased risk for CV disorders with GnRH agonists versus the GnRH antagonist degarelix.While no study has directly compared GnRH agonists versus antagonists with a primary CV outcome,one hypothesis for this observation is that GnRH agonists lead to initial surges in FSH that may negatively impact CV health,whereas antagonists do not.GnRH agonists are associated with metabolic and cognitive AEs and while data are lacking for GnRH antagonists,no differences in risk are predicted.Other common AEs with ADT include injection site reactions,which are much more common with degarelix than with GnRH agonists,which may reflect differing administration and injection techniques.Future studies are needed to further evaluate and compare the safety profiles of GnRH agonists and antagonists,especially in patients with pre-existing CV disease and other co-morbidities.Physicians should carefully evaluate benefits and risks when prescribing ADT and ensure that side effects are well managed. 展开更多
关键词 androgen antagonists metabolic syndrome prostate cancer safety
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Design,synthesis and biological estimation of 1-(benzoxazole-2-yl)piperazine and 4-(benzoxazole-2-yl)piperidine derivatives as potentialα_1-AR antagonists 认领 引用 被引量：2
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作者 Jia Bin Li Lin Xia +2 位作者 Bin Wu Tao Wang Zhen Zhou Jiang 《Chinese Chemical Letters》 SCIE CAS 2008年第10期1193-1195,共3页
Two series of 1-（benzoxazole-2-yl）piperazine （Sa-i） and 4-（benzoxazole-2-yl）piperidine compounds （10a-i） were designed, synthesized and evaluated for their α1-AR antagonistic activities. Biological assay in v... Two series of 1-（benzoxazole-2-yl）piperazine （Sa-i） and 4-（benzoxazole-2-yl）piperidine compounds （10a-i） were designed, synthesized and evaluated for their α1-AR antagonistic activities. Biological assay in vitro indicated that 10h showed slightly stronger α1-AR antagonistic activity to that of our lead compound 1. 展开更多
关键词 BPH α1-AR antagonists Benzoxazole Piperidine Piperazine
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Head-to-head comparison of H_2-receptor antagonists and proton pump inhibitors in the treatment of erosive esophagitis: A meta-analysis 认领 引用 被引量：2
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作者 Wei-HongWang Jia-QingHuang +4 位作者 Ge-FanZheng HarryHua-XiangXia Wai-ManWong Shiu-KumLam BenjaminChun-YuWong 《World Journal of Gastroenterology》 SCIE CAS 2005年第26期4067-4077,共11页
AIM: To systematically evaluate the efficacy of H2-receptor antagonists (H2RAs) and proton pump inhibitors in healing erosive esophagitis (EE).METHODS: A meta-analysis was performed. A literature search was conducted ... AIM: To systematically evaluate the efficacy of H2-receptor antagonists (H2RAs) and proton pump inhibitors in healing erosive esophagitis (EE).METHODS: A meta-analysis was performed. A literature search was conducted in PubMed, Medline, Embase, and Cochrane databases to include randomized controlled head-to-head comparative trials evaluating the efficacy of H2RAs or proton pump inhibitors in healing EE. Relative risk (RR) and 95% confidence interval (CI) were calculated under a random-effects model.RESULTS: RRs of cumulative healing rates for each comparison at 8 wk were: high dose vs standard dose H2RAs,1.17 (95%CI, 1.02-1.33); standard dose proton pump inhibitors vsstandard dose H2RAs, 1.59 (95%CI, 1.44-1.75);standard dose other proton pump inhibitors vs standard dose omeprazole, 1.06 (95%CI, 0.98-1.06). Proton pump inhibitors produced consistently greater healing rates than H2RAs of all doses across all grades of esophagitis, including patients refractory to H2RAs. Healing rates achieved with standard dose omeprazole were similar to those with other proton pump inhibitors in all grades of esophagitis.CONCLUSION: H2RAS are less effective for treating patients with erosive esophagitis, especially in those with severe forms of esophagitis. Standard dose proton pump inhibitors are significantly more effective than H2RAs in healing esophagitis of all grades. Proton pump inhibitors given at the recommended dose are equally effective for healing esophagitis. 展开更多
关键词 Erosive esophagitis H2-receptor antagonists Proton pump inhibitors Meta-analysis
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Pharmacophore-guided design,synthesis and evaluation of quinazoline-arylpiperazines as newα_1-adrenoceptor antagonists 认领 引用 被引量：4
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作者 Hao Fang Min Yong Li Lin Xia 《Chinese Chemical Letters》 SCIE CAS 2007年第1期41-44,共4页
A series of arylpiperazinesquinazoline-2,4-diamine compounds were designed and synthesized based on pharmacophore for m-selective α1-adrenoceptor antagonists and 3D chemical database searching. The in vitro functiona... A series of arylpiperazinesquinazoline-2,4-diamine compounds were designed and synthesized based on pharmacophore for m-selective α1-adrenoceptor antagonists and 3D chemical database searching. The in vitro functional analysis showed that compounds 9 and 14 showed better and similar α1-AR antagonistic activity compared with prazosin. 展开更多
关键词 α1-Adrcnoceptor Antagonists Pharmacophore-guided design
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Design and synthesis of 2-alkylbenzimidazole derivatives as novel non-peptide angiotensin Ⅱ AT1 receptor antagonists 认领 引用 被引量：1
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作者 Jin Yi Xu Qian Ran +3 位作者 Wei Yi Hua Xiao Ming Wu Qiu Juan Wang Jing Zhang 《Chinese Chemical Letters》 SCIE CAS 2007年第3期251-254,共4页
A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonis... A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonism of angiotensin H, induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9a, 9g and 9j exhibited potent antagonistic activity of AT1 receptor. 展开更多
关键词 2-Alkylbenzimidazole AT1 receptor antagonists Synthesis Hypertension
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CLINICAL COMPARISON OF THE SELECTIVE SEROTONIN_3 ANTAGONISTS RAMOSETRON AND GRANISETRON IN TREATING ACUTE CHEMOTHERAPY-INDUCED EMESIS,NAUSEA AND ANOREXIA 认领 引用 被引量：2
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作者 冯奉仪 张频 +4 位作者 何友兼 李宇红 周美珍 陈刚 李琳 《Chinese Medical Sciences Journal》 CAS 2002年第3期168-172,共5页
Feng Fengyi , Zhang Pin , He Youjian 1, Li Yuhong1 , Zhou Meizhen2 , Chen Gang2 and Li Lin2 The Cancer Hospital of the CAMS & PUMC, Beijing 1000211 The Cancer Hospital of Sun Yat Sen University of Medical Scienc... Feng Fengyi , Zhang Pin , He Youjian 1, Li Yuhong1 , Zhou Meizhen2 , Chen Gang2 and Li Lin2 The Cancer Hospital of the CAMS & PUMC, Beijing 1000211 The Cancer Hospital of Sun Yat Sen University of Medical Sciences, Guangzhou 5100602Beijing Hospital of the Ministry of Health, Beijing 100730 展开更多
关键词 HT3 antagonist ramosetron granisetronObjective. The efficacies of the selective 5 hydroxytryptamine3 (5 HT3) antagonists——ramosetron (0.3 mg) and granisetron (3 mg) in treating acute chemotherapy induced digestive system dysfunction were
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Protective Effects of Calcium Antagonists on Cadmium-induced Toxicity in Rats 认领 引用 被引量：4
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作者 YANG XIANFANG YANG YONG-NIANAbbreviation are Ca, calcium +5 位作者 CaM, calmodulin Cd, cadmium CPZ, chlorpromazine Hb, hemogobin NIMO, nimodepine NAG, N-acetyl-β-D- gluco 《Biomedical and Environmental Sciences》 SCIE CAS 1997年第4期402-407,共6页
Protective effects of calcium antagonists, chlorpromazine (CPZ) and nimodepine (NI-MO), on cadmium-induced toxicity were investigated. After giving CdCl2 (0. 44mg Cd/kg,ip), CPZ (5mg/kg, ip) or NIMO (8mg/kg, po) were ... Protective effects of calcium antagonists, chlorpromazine (CPZ) and nimodepine (NI-MO), on cadmium-induced toxicity were investigated. After giving CdCl2 (0. 44mg Cd/kg,ip), CPZ (5mg/kg, ip) or NIMO (8mg/kg, po) were administered every day to Sprague-Dawley (S. D. ) rats for a week. Then, urinary N- acetyl-β-D- glucosaminidase (NAG ), uri -nary cadmium and bloocl cadmium were measured. The accumulation of cadmium in the kid-ney cortex, content of renal calmodulin, hemoglobin and the ultrastructural damage of proxi-mal convoluted tubules of rats were examined three weeks after the last administration. Re-sults indicated that the calcium antagonists partly protected against toxic effects induced bycadmium in different manners. These data provide further evidence for the new hypothesisthat the cross effect of cadmium and calcium in calmodulin regulated systems may be responsi-ble for the mechanism of cadmium intoxication. 'The results suggested that the calcium antag-onists could be a new and promising approach in the therapy of heavy metaLinduced diseases 展开更多
关键词 Re Protective Effects of Calcium Antagonists on Cadmium-induced Toxicity in Rats
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Development of abscisic acid receptor agonists/antagonists and their application prospect in agriculture:An overview 认领 引用 被引量：1
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作者 Xianjun Tang Xiaobin Li Zhaohai Qin 《Advanced Agrochem》 CAS 2024年第1期9-25,共17页
Abscisic acid(ABA),a plant hormone,is crucial for regulating various physiological and developmental processes in plants,including adaptation to biotic and abiotic stresses.Recent advancements have significantly contr... Abscisic acid(ABA),a plant hormone,is crucial for regulating various physiological and developmental processes in plants,including adaptation to biotic and abiotic stresses.Recent advancements have significantly contributed to our understanding of ABA's biosynthetic pathway,transport,signaling pathway,and metabolism.To overcome the limitations of natural ABA,scientists have developed broad-spectrum and highly active agonists of ABA receptors.However,the practical application of these receptor agonists as agrochemicals still faces several challenges.On the other hand,some ABA antagonists have also been developed to differentiate the functional differences among various receptors more accurately.This can help design ABA agonists that can selectively activate specific physiological responses,thereby eliminating the undesired physiological effects induced by ABA.This paper aims to provide a comprehensive overview of the current ABA receptor agonists and antagonists to assist in developing novel ABA functional analogs with improved efficacy and simpler chemical structures that are suitable for agricultural applications. 展开更多
关键词 Abscisic acid(ABA) ABA receptors Receptor agonists Receptor antagonists
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Support vector classification for SAR of 5-HT3 receptor antagonists 认领 引用 被引量：1
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作者 杨善升 陆文聪 +1 位作者 纪晓波 陈念贻 《Journal of Shanghai University(English Edition)》 2006年第4期366-370,共5页
In this work, support vector classification （SVC） algorithm was used to build structure-activity relationship （SAR） model of the 5-hydroxytryptamine type 3 （5-HT3 ） receptor antagonists with 26 compounds. In a b... In this work, support vector classification （SVC） algorithm was used to build structure-activity relationship （SAR） model of the 5-hydroxytryptamine type 3 （5-HT3 ） receptor antagonists with 26 compounds. In a benchmark test, SVC was compared with several techniques of machine learning currently used in the field. The prediction performance of the model was discussed on the basis of the leave-one-out cross-validation. The results show that the accuracy of prediction of SVC model was higher than those of back propagation artificial neural network （BP ANN）, K-nearest neighbor （KNN） and Fisher methods. 展开更多
关键词 support vector classification structure-activity relationship chemometrics 5-HT3 receptor antagonists.
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The risk of bleeding of triple therapy with vitamin K-antagonists,aspirin and clopidogrel after coronary stent implantation:Facts and questions 认领 引用 被引量：1
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作者 Andrea Rubboli 《Journal of Geriatric Cardiology》 SCIE CAS CSCD 2011年第4期207-214,共8页
Background Triple therapy(TT)with vitamin K-antagonists(VKA),aspirin and clopidogrel is the recommended antithrombotic treatment following percutaneous coronary intervention with stent implantation(PCI-S)in patients w... Background Triple therapy(TT)with vitamin K-antagonists(VKA),aspirin and clopidogrel is the recommended antithrombotic treatment following percutaneous coronary intervention with stent implantation(PCI-S)in patients with an indication for oral anticoagulation.TT is associated with an increased risk of bleeding,but available evidence is flawed by important limitations,including the limited size and the retrospective design of most of the studies,as well as the rare reporting of the incidence of in-hospital bleeding and the treatment which was actually ongoing at the time of bleeding.Since the perceived high bleeding risk of TT may deny patients effective strategies,the determination of the true safety profile of TT is of paramount importance.Methods All the 27 published studies where the incidence of bleeding at various time points during follow-up has been reported separately for patients on TT were reviewed,and the weakness of the data was analyzed.Results The absolute incidence of major bleeding upon discharge at in-hospital,≤1 month,6 months,12 months and≥12 months was:3.3%±1.9%,5.1%±6.7%,8.0%±5.2%,9.0%±8.0,and 6.2%±7.8%,respectively,and not substantially different from that observed in previous studies with prolonged dual antiplatelet treatment with aspirin and clopidogrel.Conclusions While waiting for the ongoing,large-scale,registries and clinical trials to clarify the few facts and to answer the many questions regarding the risk of bleeding of TT,this treatment should not be denied to patients with an indication for VKA undergoing PCI-S provided that the proper measures and cautions are implemented. 展开更多
关键词 percutaneous coronary intervention stent bleeding oral anticoagulation vitamin K antagonists aspirin clopidogrel
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Luteinizing hormone-releasing hormone receptor agonists and antagonists in prostate cancer:effects on long-term survival and combined therapy with next-generation hormonal agents 认领 引用
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作者 Jinge Zhao Junru Chen +2 位作者 Guangxi Sun Pengfei Shen Hao Zeng 《Cancer Biology & Medicine》 SCIE CAS CSCD 2024年第11期1012-1032,共21页
Prostate cancer is a leading cause of cancer-related death in men worldwide.Luteinizing hormone-releasing hormone receptor(LHRH-R)agonists and antagonists are known to achieve castration-level testosterone suppression... Prostate cancer is a leading cause of cancer-related death in men worldwide.Luteinizing hormone-releasing hormone receptor(LHRH-R)agonists and antagonists are known to achieve castration-level testosterone suppression;however,long-term data comparing the survival benefits of these therapies are insufficient to inform treatment decisions.Furthermore,the advent of nextgeneration hormonal agents(NHAs),such as abiraterone and enzalutamide,have shifted the paradigm of managing prostate cancer.Although LHRH-R agonists and antagonists remain the cornerstone treatment across various stages of prostate cancer,they are increasingly administered with NHAs,because the combination treatment confers a survival advantage.Nevertheless,the differences in efficacy and safety profiles among various combinations of LHRH-R agonists and antagonists and NHAs remain unclear.Hence,this narrative review is aimed at providing a comprehensive overview of the long-term outcomes of various LHRH-R agonists and antagonists.Key data from major clinical studies are summarized,categorized by disease stage.LHRH-R agonists and antagonists,particularly goserelin,have demonstrated long-term survival benefits in patients with localized and locally advanced prostate cancer.The clinical outcomes of different LHRH-R agonists and antagonists in combination with NHAs have also been evaluated.Among the various combinations,goserelin plus abiraterone appears to have a manageable safety profile with relatively low rates of hot flushes and fatigue.Overall,long-term survival data and safety profiles should be considered in selecting optimal combination therapies for prostate cancer treatment. 展开更多
关键词 Luteinizing hormone-releasing hormone receptor agonists luteinizing hormone-releasing hormone receptor antagonists prostate cancer long-term survival next-generation hormonal agents
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Design,synthesis and biological evaluation of 1,4-dihydrothieno[3′,2′:5,6]thiopyrano[4,3-c]pyrazole-3-carboxylic amide derivatives as potential estrogen receptor antagonists 认领 引用
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作者 Rui Sun Jing Song +6 位作者 Si Jie Liu Hui Zhao Chun Li Yan Ai Jun Zhang Diwa Koirala Da Wei Li Chun Hu 《Chinese Chemical Letters》 SCIE CAS CSCD 2011年第3期256-259,共4页
The estrogen receptor is a target for therapeutic agents for hormone replacement in menopausal women,osteoporosis, reproductive cancers such as breast cancer,uterine cancer and prostate cancer.1,4-Dihydrothieno[3＇,2... The estrogen receptor is a target for therapeutic agents for hormone replacement in menopausal women,osteoporosis, reproductive cancers such as breast cancer,uterine cancer and prostate cancer.1,4-Dihydrothieno[3＇,2＇：5,6]thiopyrano[4,3- c]pyrazole-3-carboxylic amide derivatives were designed,synthesized and biological evaluated as potential estrogen receptor antagonists. 展开更多
关键词 Estrogen receptor antagonists Synthesis Biological activity Thiophene Pyrazole Thiopyran Piperazine
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Quantitative Stucture-Activity Relationship Studies onCalmodulin Antagonists of Alkylamino 1,2-Diphenylethvl-ene Compounds 认领 引用
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作者 雷小平 李重华 钟海振 《Journal of Chinese Pharmaceutical Sciences》 CAS 1996年第4期169-173,共5页
从新的先导化合物6－氨基1，2－二苯乙烯－1出发，研究了15个烷氨基1，2－二苯乙烯类钙调素拮抗剂的结构与活性之间的关系。发现：顺式构型的活性一般比反式构型强，而双键还原的化合物活性更低。从芳香亲脂中心到碱性中心之间的烷基链... 从新的先导化合物6－氨基1，2－二苯乙烯－1出发，研究了15个烷氨基1，2－二苯乙烯类钙调素拮抗剂的结构与活性之间的关系。发现：顺式构型的活性一般比反式构型强，而双键还原的化合物活性更低。从芳香亲脂中心到碱性中心之间的烷基链长度增加时，拮抗活性随之增强。QSAR分析显示：苯环上具较大脂水分配系数及给电子的取代基时拮抗活性可提高。 展开更多
关键词 Calmodulin antagonists QSAR Hansch analysis
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Effect of endothelin-1 receptor antagonists on histological and ultrastructural changes in the pancreas and trypsinogen activation in the early course of caerulein-induced acute pancreatitis in rats 认领 引用 被引量：4
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作者 Anna Andrzejewska Jan W.Dlugosz Albert Augustynowicz 《World Journal of Gastroenterology》 SCIE CAS 2005年第8期1115-1121,共7页
AIM: To assess the effect of non-selective ETA/B (LU 302872)and selective ETA (LU 302146) antagonist on pancreatic histology and ultrastructure of acinar cells in connection with trypsinogen activation in early caerul... AIM: To assess the effect of non-selective ETA/B (LU 302872)and selective ETA (LU 302146) antagonist on pancreatic histology and ultrastructure of acinar cells in connection with trypsinogen activation in early caerulein-induced AP.METHODS: Male Wistar rats with caerulein-induced AP,lasting 4 h, were treated i.p. with 10 and 20 mg/kg b.w.of each antagonist. Edema, inflammatory infiltration,necrosis and vacuolization of acinar cells in the pancreas were scored at 0-3 scale. Free active trypsin (FAT), total potential trypsin (TPT) after activation with enterokinase,and index of trypsinogen activation (%FAT/TPT) were assayed in pancreatic homogenates.RESULTS: In untreated AP, the edema, inflammatory infiltration, necrosis and vacuolization increased as compared to control healthy rats (P＜0.01). None of the treatment exerted any meaningful effect on the edema and inflammatory infiltration. The selective antagonist increased slightly the necrosis score to 0.82±0.06 at higher dose (P＜0.05) vs 0.58±0.06 in untreated AP. The nonselective antagonist increased slightly the vacuolization score to 2.41±0.07 at higher dose (P＜0.01) vs 1.88±0.08in untreated AP. The decrease in the number of zymogen granules, disorganization of endoplasmic reticulum,autophagosomes and cytoplasmic vacuoles were more prominent in treated AP than in untreated AP groups.%FAT/TPT in untreated AP increased about four times (18.4±3.8 vs4.8±1.3 in control group without AP, P＜0.001).Treatment of AP with both antagonists did not affect significantly augmented trypsinogen activation.CONCLUSION: The treatment with endothelin-1 receptors (non-selective ETA/B and selective ETA) antagonists has essential effect neither on the edema and inflammatory infiltration nor on trypsinogen activation observed in the early course of caerulein-induced AP. Nevertheless a slight increase of the necrosis and vacuolization score and some of the ultrastructural data could suggest the possibility of their undesired effects in caerulein-induced AP at investigated doses. 展开更多
关键词 Acute pancreatitis Caerulein Endothelin-1 receptors antagonists Ultrastructure Trypsin
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Medical therapy for clinical benign prostatic hyperplasia:α1 Antagonists,5α reductase inhibitors and their combination 认领 引用 被引量：4
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作者 Cheuk Fan Shum Weida Lau Chang Peng Colin Teo 《Asian Journal of Urology》 2017年第3期185-190,共6页
Medical therapy for clinical benign prostatic hyperplasia(BPH)has advanced significantly in the last 2 decades.Many new a1 antagonists and 5a reductase inhibitors(5ARi)are now commercially available.The practicing uro... Medical therapy for clinical benign prostatic hyperplasia(BPH)has advanced significantly in the last 2 decades.Many new a1 antagonists and 5a reductase inhibitors(5ARi)are now commercially available.The practicing urologist must decide on the most appropriate medication for his patients,taking into consideration various factors like efficacy,dosing regime,adverse effects,cost,patient’s socioeconomic background,expectations,drug availability and his own clinical experience.The use of combination therapy added further to the complexity in clinical judgment when prescribing.We highlight some of the key points in prescribing a1 antagonists,5ARi and their combination,based on our viewpoints and experience as urologists in an Asian clinical setting. 展开更多
关键词 5αReductase inhibitors Adrenergicα1 receptor antagonists Drug therapy Combination Prostatic hyperplasia
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Spectrofluorimetric method for determination of some angiotensin II receptor antagonists 认领 引用 被引量：2
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作者 Salwa R. El-Shaboury Samiha A. Hussein +1 位作者 Niveen A. Mohamed Mohamed M. El-Sutohy 《Journal of Pharmaceutical Analysis》 CAS 2012年第1期12-18,共7页
A simple, rapid, accurate and highly sensitive spectrofluorimetric method has been developed for determination of some angiotensin II receptor antagonists (AIIRA’s), namely Losartan potassium (Los-K), Irbesartan (Irb... A simple, rapid, accurate and highly sensitive spectrofluorimetric method has been developed for determination of some angiotensin II receptor antagonists (AIIRA’s), namely Losartan potassium (Los-K), Irbesartan (Irb), Valsartan (Val) and Candesartan cilexetil (Cand) in pure forms as well as in their pharmaceutical dosage forms. All the variables affecting the relative fluorescence intensity (RFI) were studied and optimized. Under the optimum conditions, linear relationships with good correlation coefflcients (0.9982–0.9991) were obtained over the concentration range from 0.006 mg/mL to 1.7 mg/mL. Good accuracy and precision were successfully obtained for the analysis of tablets containing each drug alone or combined with hydrochlorothiazide (HCTZ) without interferences from the co-formulated HCTZ or the additives commonly present in tablets. 展开更多
关键词 Angiotensin II receptor antagonists Spectrofluorimetry Determination
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Synthesis of thiourea derivatives as CCR4 antagonists 认领 引用 被引量：1
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作者 Fang Zhao Jun Hai Xiao +1 位作者 Ying Wang Song Li 《Chinese Chemical Letters》 SCIE CAS 2009年第3期296-299,共4页
A series of thiourea derivatives have been synthesized. Their structures were confirmed by MS and 1H NMR. Several compounds showed potent activities as antagonists of CCR4 receptor.
关键词 CCR4 antagonists Thiourea derivatives Synthesis
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Cost Effectiveness of Sodium-Glucose Cotransporter 2 Inhibitors Compared with Mineralocorticoid Receptor Antagonists among Patients with Heart Failure and a Reduced Ejection Fraction 认领 引用 被引量：1
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作者 Jingchaun Guo Matthew R.Petersen +3 位作者 Huilin Tang Lauren E.Meece Hui Shao Mustafa M.Ahmed 《Cardiovascular Innovations and Applications》 2023年第1期279-286,共8页
Objective:Sodium-glucose cotransporter 2 inhibitors(SGLT2i)are approved for heart failure with reduced ejection fraction(HFrEF).However,their cost-effectiveness remains unknown.We aimed to compare the cost-effectivene... Objective:Sodium-glucose cotransporter 2 inhibitors(SGLT2i)are approved for heart failure with reduced ejection fraction(HFrEF).However,their cost-effectiveness remains unknown.We aimed to compare the cost-effectiveness of SGLT2i versus mineralocorticoid antagonists(MRAs).Methods:Data from the RALES,EPHESUS,EMPHASIS,DAPA-HF,and EMPEROR-Reduced trials were includ-ed.We calculated the risk-ratio(RR)for a composite of cardiovascular death or heart failure hospitalization(CV death-HHF),all-cause mortality,and heart failure hospitalization(HHF)between MRAs and SGLT2i.A Markov model was developed to simulate the progression of HFrEF over 5 years.The primary outcome was incremental cost-effectiveness ratio(ICER),measured by cost per quality-adjusted life-year(QALY)gained.Results:We observed a similar benefit in CV death-HHF(RR 1.04;95%CI 0.82–1.31),all-cause mortality(RR 0.91;95%CI 0.78–1.06),and HHF(RR 1.05;95%CI 0.84–1.31)between MRAs and SGLT2i.In a 5-year model,no difference in survival was observed between treatments.MRAs were associated with lower cost($63,135.52 vs.$80,365.31)and more QALYs gained per patient(2.53 versus 2.49)than SGLT2i.The ICER for SGLT2i versus MRAs was$-172,014.25/QALY,in favor of MRAs.Conclusion:MRAs and SGLT2i provided similar benefits;however,MRAs were a more cost-effective treatment than SGLT2i. 展开更多
关键词 Sodium glucose transporter-2 inhibitors Heart failure Mineral corticoid receptor antagonists Costeffectiveness
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