受体激动剂 Ro5-4864 抑制大鼠心肌细胞线粒体通透性转换 17 过外膜,高度膨胀的基质导致线粒体内膜的嵴伸 展,进而外膜破裂,释放出位于膜间隙的促凋亡分 子如 Cyto C 、Smac/DIABIO ( 一种新型线粒体蛋 白) 、凋亡诱导因子(apoptosis inducing factor, AIF)、 核酸内切酶(Endo G) 、Htra2/Omi 等,通过 ...
Ro5-4864 also suppressed cell proliferation, as well as adenosine triphosphate and lactate production, during T cell activation. Moreover, the inhibitory effects of Ro5-4864 on T cell responses were conserved in TSPO-deficient cells. Our results suggest that Ro5-4864 inhibits CH responses by ...
结果:SAH可导致小鼠体重减轻,引起神经炎症反应及运动神经功能障碍.Ro5-4864缓解了SAH后小鼠体重的丢失,减少了脑组织含水量和降低了TNF-α的表达,一定程度地促进了神经功能恢复,但不能减少IL-1β的表达.结论:TSPO配体Ro5-4864具有一定的神经保护功能,可缓解小鼠SAH后体重下降和脑组织炎症因子升高水平,并改善小鼠神经...
Ro5-4864 suppressed pro-inflammatory MC effector functions in response to antigen (Ag) (degranulation/cytokine production) and LPS and SCF (cytokine production), whereas clonazepam was inactive. Signaling pathway analyses revealed inhibitory effects of Ro5-4864 on Ag-triggered production of reactive ...
Ro5-4864缓解了SAH后小鼠体重的丢失,减少了脑组织含水量和降低了TNF-α的表达,一定程度地促进了神经功能恢复,但不能减少IL-1β的表达。结论:TSPO配体Ro5-4864具有一定的神经保护功能,可缓解小鼠SAH后体重下降和脑组织炎症因子升高水平,并改善小鼠神经功能缺损,为临床对SAH后的综合治疗提供实验依据。 展开 ...
Ro5-4864 suppressed pro-inflammatory MC effector functions in response to antigen (Ag) (degranulation/cytokine production) and LPS and SCF (cytokine production), whereas clonazepam was inactive. Signaling pathway analyses revealed inhibitory effects of Ro5-4864 on Ag-triggered production of reactive ...
Nefiracetam作用于Ro 5-4864引起的抽搐,是GABAergic,胆碱及单胺类的神经系统增强剂。Phase 2。 靶点(IC50 & Targe) GABAR 体外研究 Nefiracetam在1 μM浓度下增加2倍钙通道电流的长效组分,而不影响瞬变组分。[2] Nefiracetam在亚微摩尔浓度下(0.01–0.1 μM)诱导Ach激发电流的短期抑制,在微摩尔浓度下(1...
Ro5-4864 and PK11195, prototypical synthetic ligands of translocator protein 18 kDa (TSPO), have shown anti-inflammatory effects in several models of inflammatory diseases; however, their biochemical mechanisms remain poorly understood. Nod-like receptor family, pyrin domain containing 3 (NLRP3) infl...
The present study was designed to investigate the effects of diazepam, a benzodiazepine (BZ) with high affinity to central BZ receptors and moderate affinity to mitochondiral BZ receptors, and of Ro 5-4864 and PK 11195, ligands specific for mitochondrial BZ receptors, on cardiac function in the...
Characterization of peripheral-type benzodiazepine binding sites in brain using [3H]Ro 5-4864. The binding of [3H]Ro 5-4864 to the peripheral-type benzodiazepine binding site in brain is characterized. The binding is saturable, high-affinity (KD = 1... PJ Marangos,J Patel,JP Boulenger,.....