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1.
目的 探讨美沙拉嗪肠溶片联合蒙脱石散治疗溃疡性结肠炎的临床治疗效果。方法 选取2017年1月-2017年12月在江苏省滨海县人民医院治疗的溃疡性结肠炎患者80例作为研究对象,将患者随机分为对照组和观察组,每组各40例。对照组患者给予柳氮磺吡啶肠溶片,8片/次,3次/d,另给予蒙脱石散,将蒙脱石散置入50 mL的温水内,摇匀后服用,1次/d。观察组患者口服美沙拉嗪肠溶片,4次/d,4片/次;联合蒙脱石散,服用方法同对照组。所有患者均接受8周连续治疗。观察两组患者的临床治疗效果及不良反应发生率,并比较两组治疗前后血清样本中肿瘤坏死因子-α(TNF-α)和白细胞介素-6(IL-6)的水平。结果 治疗后,观察组患者的临床治疗有效率为92.50%,对照组患者的临床治疗有效率为72.50%,两组比较差异具有统计学意义(P<0.05)。治疗前,两组患者的血清TNF-α及IL-6水平相比,差异均无统计学意义;治疗后,两组血清TNF-α、IL-6水平均显著降低,同组治疗前后比较差异有统计学意义(P<0.05);且观察组患者的血清TNF-α及IL-6水平均显著低于对照组,差异具有统计学意义(P<0.05)。观察组患者治疗期间不良反应发生率为12.50%,对照组患者治疗期间不良反应发生率为32.50%,差异具有统计学意义(P<0.05)。结论 美沙拉嗪肠溶片联合蒙脱石散治疗溃疡性结肠炎的临床治疗效果较好,安全性较高。  相似文献   

2.
目的 探讨谷氨酰胺胶囊联合美沙拉秦肠溶片治疗溃疡性结肠炎的效果。方法 回顾性选取河南省洛阳市偃师人民医院2020年12月—2021年12月收治的溃疡性结肠炎患者137例为研究对象,根据治疗方案分为对照组(n=69)和试验组(n=68),对照组给予美沙拉秦肠溶片治疗,每次4片,每天3次,连续治疗1个月;试验组在对照组基础上加用谷氨酰胺胶囊治疗,每次0.5 g,每天3次,连续治疗1个月。对比两组患者治疗前后血清C反应蛋白(CRP)、血沉(ESR)、胰岛素生长因子-Ⅰ(IGF-Ⅰ)、白细胞介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)、转化生长因子-β1(TGF-β1)及溃疡性结肠炎活动指数Sutherland评分,观察临床疗效及不良反应。结果 治疗前,试验组和对照组的血清CRP、ESR、IGF-Ⅰ、IL-6、TNF-α、TGF-β1测定值差异无统计学意义(P>0.05);治疗后,两组患者血清CRP、ESR、IL-6、TNF-α测定值均较治疗前显著降低(P<0.05),且治疗后试验组的血清CRP、ESR、IL-6、TNF-α测定值均显著低于对照组(P<0.05);治疗后,两组患者血清IGF-Ⅰ、TGF-β1测定值均较治疗前显著升高(P<0.05),且试验组的IGF-Ⅰ、TGF-β1测定值均显著高于对照组(P<0.05);治疗前,试验组和对照组的Sutherland评分差异无统计学意义(P>0.05);治疗后,两组Sutherland评分均较治疗前显著降低(P<0.05),且试验组的Sutherland评分显著低于对照组(P<0.05);治疗后,试验组的整体疗效分布优于对照组,差异具有统计学意义(P<0.05);治疗过程中,试验组的不良反应发生率4.41%与对照组的5.80%对比,差异不具有统计学意义(P>0.05)。结论 谷氨酰胺胶囊联合美沙拉秦肠溶片治疗溃疡性结肠炎较单用美沙拉秦肠溶片具有更好的临床效果。  相似文献   

3.
目的 探讨消糜栓与氟康唑片联合治疗念珠菌性阴道炎的临床疗效。方法 选择2021年2月—2021年8月在濮阳市油田总医院治疗的97例念珠菌性阴道炎患者,随机分为对照组(49组)和治疗组(48组)。对照组患者口服氟康唑片,150 mg/次,1次/d。在对照组的基础上,治疗组阴道给予消糜栓,1粒/次,1次/d。两组用药7 d观察治疗效果。观察两组患者临床疗效,比较治疗前后两组患者症状改善时间,血清白细胞介素-6(IL-6)、γ干扰素(IFN-γ)、肿瘤坏死因子-α(TNF-α)、C反应蛋白(CRP)水平,及不良反应情况。结果 治疗后,治疗组临床有效率为97.91%,明显高于对照组的81.63%(P<0.05)。经治疗,治疗组症状改善时间均明显早于对照组(P<0.05)。治疗后,两组患者血清IL-6、IFN-γ、TNF-α、CRP水平均明显降低(P<0.05);且治疗组IL-6、IFN-γ、TNF-α、CRP水平均明显低于对照组(P<0.05)。治疗组不良反应发生率为6.25%,明显低于对照组的14.29%(P<0.05)。结论 对于念珠菌性阴道炎治疗,采用氟康唑片与消糜栓治疗效果确切,并可以调节血清炎性因子水平,能有效降低复发率,且安全有效。  相似文献   

4.
目的 探讨瘀血痹胶囊联合艾瑞昔布片治疗膝骨关节炎的临床疗效。方法 选取2020年3月—2022年3月中国人民解放军联勤保障部队第九〇四医院收治的130例膝骨关节炎患者,根据随机数字表法将所有患者分为对照组和治疗组,每组各65例。对照组餐后温水送服艾瑞昔布片,1片/次,2次/d。治疗组在对照组基础上口服瘀血痹胶囊,6粒/次,3次/d。两组患者连续用药8周。观察两组患者的临床疗效,采用视觉模拟评分法(VAS)评估两组患者的疼痛程度,采用改良版西安大略和麦克马斯特大学骨关节炎指数量表(WOMAC)评估两组患者的膝关节功能,比较两组患者治疗前后血清炎症因子白介素-1β(IL-1β)、白细胞介素-6(IL-6)、肿瘤坏死因子-α(TNF-α)、C反应蛋白(CRP)水平。结果 治疗后,治疗组总有效率(95.38%)高于对照组(84.62%),差异有统计学意义(P<0.05)。治疗后,两组VAS、WOMAC评分均显著下降(P<0.05),且治疗组VAS、WOMAC评分均明显低于对照组,差异有统计学意义(P<0.05)。治疗后,两组血清IL-1β、IL-6、TNF-α、CRP水平均显著下降(P<0.05),且治疗组血清IL-1β、IL-6、TNF-α、CRP水平低于对照组,差异具有统计学意义(P<0.05)。结论 瘀血痹胶囊联合艾瑞昔布片治疗膝骨关节炎具有较好的临床疗效,可有效缓解患者疼痛程度,改善膝关节功能,减轻炎症反应,且安全性较好。  相似文献   

5.
目的 探讨蒲地蓝消炎口服液联合罗红霉素治疗小儿急性化脓性扁桃体炎的临床疗效。方法 选取2017年9月-2019年9月在郑州大学附属儿童医院儿科住院治疗的急性化脓性扁桃体炎患儿116例为研究对象,随机分为对照组和治疗组,每组各58例。对照组饭前1 h或饭后4 h口服罗红霉素分散片,2.5 mg/(kg·次),2次/d。治疗组在对照组治疗基础上口服蒲地蓝消炎口服液,10 mL/次,3次/d。两组患儿均连续治疗7 d。观察两组患儿的临床疗效;记录患儿临床症状消失时间;比较治疗前后患儿血清白细胞介素6(IL-6)、IL-8、IL-1β、IL-18、肿瘤坏死因子α(TNF-α)、C反应蛋白(CRP)水平。结果 治疗后,治疗组总有效率96.55%,显著高于对照组81.03%(P<0.05)。治疗后,治疗组患儿咽痛消失时间、脓点消失时间、退热时间、扁桃体恢复正常时间均显著短于对照组(P<0.05)。治疗后,治疗组患儿血清IL-6、IL-1β、IL-18、TNF-α、CRP水平均较治疗前显著降低(P<0.05);治疗后,治疗组这些炎性因子水平显著低于对照组(P<0.05)。治疗组不良反应发生率是6.89%,显著低于对照组的17.24%(P<0.05)。结论 蒲地蓝消炎口服液联合罗红霉素治疗小儿急性化脓性扁桃体炎具有较好的临床疗效,可有效缩短临床症状时间,降低炎性因子水平,具有一定的临床推广应用价值。  相似文献   

6.
目的 探讨丙卡特罗联合地塞米松磷酸钠治疗儿童支气管哮喘急性发作的临床研究。方法 选择2021年1月—2022年1月在南通市海门区人民医院诊疗的80例支气管哮喘急性发作患儿,随机分对照组(40例)和治疗组(40例)。对照组患儿静脉滴注地塞米松磷酸钠注射液,每次0.5 mg/kg,1次/d。治疗组在对照组的基础上口服盐酸丙卡特罗口服溶液,5 mL/次,2次/d。两组患儿连续治疗5 d。观察两组患儿临床疗效,比较治疗前后两组患儿症状好转时间,及血清白细胞介素-1β(IL-1β)、白细胞介素-17(IL-17)、肿瘤坏死因子-α(TNF-α)、C反应蛋白(CRP)水平。结果 治疗后,治疗组临床有效率为97.50%,明显高于对照组77.50%(P<0.05)。治疗后,治疗组症状好转时间均明显早于对照组(P<0.05)。治疗后,两组患儿IL-1β、IL-17、TNF-α、CRP水平均明显降低,且治疗组明显均低于对照组(P<0.05)。结论 地塞米松磷酸钠联合盐酸丙卡特罗治疗支气管哮喘急性发作患儿效果明显,可有效改善支气管炎症反应,促进机体免疫力增加。  相似文献   

7.
卢谦  叶少武  黄河 《现代药物与临床》2022,37(10):2268-2271
目的 探讨磺达肝癸钠与美托洛尔联合治疗老年不稳定型心绞痛的临床疗效。方法 选择2020年1月—2022年1月在梧州市人民医院治疗的102例心绞痛患者,根据随机数字表法分为对照组和治疗组,每组各51例。对照组口服酒石酸美托洛尔片,25 mg/次,2次/d。在对照组基础上,治疗组皮下注射磺达肝癸钠注射液,2.5 mg/次,1次/d。两组患者治疗7 d。观察两组患者临床疗效,比较治疗前后两组患者症状改善时间、心绞痛发作次数和持续时间,血清因子C反应蛋白(CRP)、白细胞介素-18(IL-18)、肿瘤坏死因子-α(TNF-α)和白细胞介素-6(IL-6)水平。结果 治疗后,治疗组总有效率(98.04%)明显高于对照组有效率(82.35%,P<0.05)。治疗后,治疗组症状改善时间均明显早于对照组(P<0.05)。治疗后,两组心绞痛发作次数、持续时间较治疗前均下降(P<0.05),且治疗组明显低于对照组(P<0.05)。治疗后,两组血清因子IL-6、IL-18、TNF-α、CRP水平较治疗前均明显降低(P<0.05),且治疗组的IL-6、IL-18、TNF-α、CRP水平均低于对照组(P<0.05)。结论 磺达肝癸钠联合美托洛尔治疗老年不稳定型心绞痛效果显著,可降低发作次数,有效降低炎性因子,且安全性高。  相似文献   

8.
汪洋  马民玉 《现代药物与临床》2020,35(10):2002-2005
目的 探讨风湿祛痛胶囊联合柳氮磺吡啶肠溶片治疗强直性脊柱炎的临床疗效。方法 选取2018年11月-2020年1月郑州大学第一附属医院收治的90例强直性脊柱炎患者,将所有患者根据数字表法随机分为对照组和治疗组,每组各45例。对照组口服柳氮磺吡啶肠溶片,第1周为2片/次,第2周为3片/次,第3周为4片/次,均为2次/d。治疗组在对照组的基础上口服风湿祛痛胶囊,5粒/次,3次/d。两组患者均治疗8周。观察两组患者临床疗效,比较两组的巴氏强直性脊柱炎活动指数(BASDAI)评分、视觉模拟评分法(VAS)评分、巴氏强直性脊柱炎功能指数(BASFI)评分以及血清炎症因子水平。结果 治疗后,治疗组的总有效率88.89%高于对照组68.89%(P<0.05)。治疗后,两组巴氏强直性脊柱炎活动指数(BASDAI)、巴氏强直性脊柱炎功能指数(BASFI)、VAS评分均较治疗前下降(P<0.05),且治疗组BASDAI、BASFI、VAS评分低于对照组(P<0.05)。治疗后,两组血清C反应蛋白(CRP)、肿瘤坏死因子-α(TNF-α)、白细胞介素-1β(IL-1β)水平均显著下降(P<0.05),且治疗组血清CRP、TNF-α、IL-1β水平低于对照组(P<0.05)。结论 风湿祛痛胶囊联合柳氮磺吡啶肠溶片治疗强直性脊柱炎具有较好的临床疗效,可有效改善患者临床症状,降低CRP、TNF-α、IL-1β水平。  相似文献   

9.
目的 探讨芪倍合剂联合美沙拉嗪治疗活动期溃疡性结肠炎的临床疗效和其对Th17、Treg细胞及其相关细胞因子水平的影响。方法 选取2019年1月—2019年12月于新乡医学院第一附属医院就诊的142例活动期溃疡性结肠炎患者作为研究对象,将所有患者随机分为对照组和观察组,每组各71例。对照组口服美沙拉嗪肠溶片,1 g/次,4次/d;观察组在对照组治疗的基础上口服芪倍合剂,50 mL/次,3次/d。两组疗程均为8周。观察两组患者的临床疗效,同时比较两组治疗前后的Mayo评分、Baron评分、Th17细胞、Treg细胞、Th17/Treg细胞比值、白细胞介素(IL)-17、IL-23、转化生长因子(TGF-β)和IL-10水平。结果 治疗后,对照组和观察组的总有效率分别为81.69%、94.36%,两组总有效率比较差异具有统计学意义(P<0.05)。治疗后,两组Mayo评分和Baron评分均显著降低(P<0.05);且观察组Mayo评分和Baron评分显著低于对照组(P<0.05)。治疗后,两组患者Th17细胞、Th17/Treg细胞比值水平均显著下降,而Treg细胞显著升高(P<0.05)。治疗后,与对照组相比,观察组Th17细胞和Th17/Treg细胞比值显著降低,而Treg细胞显著升高(P<0.05)。治疗后,两组血清IL-17和IL-23水平显著降低,而TGF-β和IL-10水平显著升高(P<0.05)。治疗后,观察组血清IL-17、IL-23水平显著低于对照组,而TGF-β和IL-10水平显著高于对照组(P<0.05)。结论 芪倍合剂联合美沙拉嗪对活动期溃疡性结肠炎临床疗效较好,治疗安全性高,能有效改善患者的临床症状,可能机制与其能显著改善Th17/Treg细胞平衡有关。  相似文献   

10.
目的 探讨香连化滞丸联合美沙拉嗪治疗溃疡性结肠炎的临床疗效。方法 纳入驻马店市中医院于2020年1月—2021年6月收治的98例溃疡性结肠炎患者为研究对象,随机分为对照组和治疗组,每组各49例。对照组患者口服美沙拉嗪肠溶片,1 g/次,4次/d,治疗组在对照组的基础口服香连化滞丸,12 g/次,2次/d。两组均治疗12周。观察两组患者临床疗效,比较治疗前后两组患者临床症状缓解时间,二胺氧化酶、D-乳酸、超氧化物歧化酶、丙二醛、转化生长因子-β(TGF-β)、白细胞介素-10(IL-10)和IL-17水平。结果 治疗后,对照组和治疗组总有效率分别为81.63%、95.92%,两组比较差异具有统计学意义(P<0.05)。治疗后,与对照组相比,治疗组血便消失平均时间及腹泻次数至少降低50%所需时间显著缩短(P<0.05)。治疗后,两组二胺氧化酶、D-乳酸、丙二醛和IL-17水平均显著降低,超氧化物歧化酶、TGF-β和IL-10水平显著升高(P<0.05),且治疗组这些指标显著好于对照组(P<0.05)。结论 香连化滞丸联合美沙拉嗪治疗溃疡性结肠炎临床疗效显著,能显著改善溃疡性结肠炎患者的肠道黏膜屏障功能、氧化应激水平及Th17/Treg细胞失衡。  相似文献   

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We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.  相似文献   

13.
Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.
Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.
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16.
Lung disease and PKCs   总被引:1,自引:0,他引:1  
The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.  相似文献   

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This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.  相似文献   

19.
Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.  相似文献   

20.
Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.  相似文献   

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