PPARy 改善糖脂代谢机制-changPPT.pptxVIP

PPARγ 文献阅读报告目录替米沙坦部分激活PPARγ美卡素和吡格列酮结构相似替米沙坦，唯一治疗剂量下激活PPARγ的ARBRAS PPARγ 改善高血压-糖尿病机制美卡素双重抗动脉粥样硬化作用激活PPARγ可以调低AT1受体表达激活PPARγ带来益处替米沙坦和传统PPARγ激动剂不同，没有水钠潴留，体重增加副反应It should be emphasized that telmisartan belongs to acategory of molecules known as selective PPAR gammamodulators (SPPARMs) [70,71]. The SPPARMs differ from conventional PPARa activators such as rosiglitazone and pioglitazone in a number of important respects. Rosiglitazone, pioglitazone and other conventional PPARa activators typically function as full agonists of the receptor and affect the expression of a very broad range of genes, whereas SPPARMs, such as telmisartan, function as partial agonists, with more restricted effects on gene expression [50,71]. SPPARMs influence the expression of some, but not all, of the same target genes regulated by conventional PPARa activators [50,71]. The overlapping, yet differential, effects on gene expression of SPPARMs versus conventional PPAR ligands may mediate some of the similarities and differences in their biologic effects. For example, in rodent models of insulin resistance and obesity induced by administration of high fat, high carbohydrate diets, both conventional PPARa activators and SPPARMs can improve carbohydrate and lipid metabolism [50,71]. However, in these models the onventional PPARa activators also promote weight gain and accumulation of body fat, whereas SPPARMs such as telmisartan and nTZDpa (an experimental Merck compound) do not. In fact, both telmisartan and nTZDpa appear to attenuate diet-induced increases in weight gain and body fat independent of effects on energy ntake (T. Kurtz, unpublished observations) [50,71].替米沙坦部分激动PPARγ,没有体重增加，水钠潴留的副作用对于高血压合并糖尿病 : 一石二鸟?目录替米沙坦通过阻断RAAS 和激活PPARγ双途径，改善内皮功能（老年人）替米沙坦通过阻断RAAS 和激活PPARγ双途径，增加NO释放（老年人）对于原发性高血压患者，替米沙坦改善动脉僵硬度替米沙坦改善高血压合并糖尿病患者内皮功能替米沙坦比厄贝沙坦更多改善胰岛素抵抗，瘦素，TNF--α目录降低FPG FPI HOMA-IR HbA1c,替米沙坦优于氯沙坦替米沙坦对比缬沙坦减少葡萄糖和甘油三酯 水平替米沙坦可以降低血糖，这和剂量相关替米沙坦改善脂代谢Effect of Telmisartan on Cholesterol Levels in Patientswith