2017年5月11日 · Alpha-7 nicotinic acetylcholine receptor (α7-nAChR) agonists can prevent glutamate-induced excitotoxicity in cultured retinal ganglion cells (RGCs). However, the neuroprotective effects and the...

2023年3月12日 · In this study, PNU-282987 activated α7-nAChRs in endothelial cells, resulting in the perinuclear accumulation of eNOS and increased NO production, which was inhibited by MLA. In endothelial cells, inactivated eNOS binds to caveolin-1 located in the plasma membrane.

目的:阻塞性睡眠呼吸暂停(obstructive sleep apnea,OSA)是指睡眠过程中反复出现上呼吸道阻塞的一种睡眠障碍,可导致血氧饱和度反复降低,睡眠片段化,交感神经自主活动增强.OSA与全身多系统疾病相关,包括认知功能障碍,高血压,糖尿病,致死性和非致死性冠状动脉事件 ...

To validate the specific effects of α7nAchR agonists, subacute MPTP mice were pretreated with methyllycaconitine (MLA), a selective α7nAchR antagonist before GTS-21 administration. Pretreatment with MLA abolished the GTS-21-elicited behavioral recovery, α-syn clearance, and anti-inflammatory effects in the brain and gut.

Results: α7nAChR stimulation improved neurological outcome and reduced brain edema at 24 and 72 hours after surgery (P<0.05 compared with vehicle). Furthermore, PHA-543613 treatment increased p-Akt and decreased p-GSK-3β and CC3 expressions in the ipsilateral hemisphere (P<0.05, respectively), which was reversed by MLA and wortmannin.

2022年6月22日 · PNU-282987 treatment remarkably improved systolic function by increasing LVEF, LVFS and IVS (d, s) at 7 and 30 days after ICH. However, MLA could reverse this effect at 30 days after ICH . It also exhibits significant increases in LVID (d, s) and LV volume (d,s) in ICH mice at 7 and 30 days after ICH compared with controls.

2015年3月26日 · Our results showed that MLA (Fig. 3A1–C1) or DhβE (Fig. 3A2–C2) partially reduced nicotinic enhancement on γ power, but a combination of both antagonists blocked the nicotinic effect (Fig ...

To validate the specific effects of α7nAchR agonists, subacute MPTP mice were pretreated with methyllycaconitine (MLA), a selective α7nAchR antagonist before GTS-21 administration. Pretreatment with MLA abolished the GTS-21-elicited behavioral recovery, α-syn clearance, and anti-inflammatory effects in the brain and gut.

PNU-282987 (free base) (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a K i of 27 nM. PNU-282987 has α7 nAChR agonist activity with an EC 50 of 154 nM. PNU-282987 also has inhibition for the 5-HT 3 receptor with an IC 50 value of 4541nM.

2021年1月25日 · We found that PNU-282987 significantly improved the motor deficits induced by 6-OHDA, reduced the loss of TH in the SN, suppressed the overactivation of GFAP+ cells and expression of related inflammatory cytokines, and increased the number of Foxp3+ cells.