glial

TGN-020 是一种属于 alkyl chain 类的 PROTAC linker，可用于 PROTAC 的合成分子。TGN020 是一种选择性水通道蛋白 4 (AQP4) 抑制剂，IC50为 3.1 μM。TGN020 减轻大鼠脊髓压迫损伤后的水肿并抑制神经胶质瘢痕的形成。

PLX5622 是一种 CSF1R 抑制剂 (IC50=0.016 µM)，具体选择性、口服活性和血脑屏障通透性。PLX5622 可以引起持续和特异性的小胶质细胞的消除。

Geranylgeraniol (FT0626663) 是一种类异戊二烯，存在于水果、蔬菜和谷物中，包括大米。 Geranylgeraniol (FT0626663) 抑制生长并诱导各种肿瘤细胞的凋亡。 Geranylgeraniol (FT0626663) 保护单核细胞免受他汀类药物诱导的细胞毒性并抑制分枝杆菌的生长。

Mulberrofuran C(桑葚呋喃 C)是存在于Morus alba中的苯并呋喃，对Aβ₁₋₄₂自聚集、tau蛋白聚集、AChE具有抑制作用，具有抗氧化活性和神经保护作用，具有抗阿尔茨海默病的潜力。

TRC051384 是一种热休克蛋白70 (HSP70) 诱导剂，可减少中风相关的神经元损伤并增加短暂性缺血性中风大鼠模型的存活率，激活热休克因子-1 并导致分子伴侣和抗炎活性升高，增强神经元和神经胶质细胞中 Hsp72 的表达。

MW01-2-151SRM 是一种新型可穿过血脑屏障的小分子小胶质细胞活化抑制剂，具有抗神经炎作用，可减弱神经炎症模型中的神经胶质细胞因子上调，可用研究创伤性脑损伤、阿尔茨海默病和海藻氨酸毒性。

Methyl eugenol (4-allylveratrole) 是一种苯丙类化合物，存在于植物叶子、果实、根茎中，当植物相应的部位因食草动物进食而受损时，就会释放。它可用于消灭雄性东方果蝇。

O-PHOSPHO-L-SERINE 是丝氨酸和磷酸的酯，是人类生物流体中的正常代谢物。O-phospho-L-serine 是一种吞噬抑制剂，抑制光损伤后的神经胶质细胞增殖和锥体细胞再生。

Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜，具有抗肿瘤作用。它通过调节PI3K Akt 信号通路抑制 GLI1 的核易位，诱导骨肉瘤凋亡。

BT-13 是一种胶质细胞源性神经营养因子 (GDNF) 受体 RET 的选择性激动剂，独立于 GDNF 配体发挥作用，能够促进体外感觉神经元神经突生长，减少大鼠神经病变的发生。

BT18 是一种功能类似于胶质细胞源神经营养因子的分子模拟物。它能够影响 GDNF 家族受体 GFRα1 和 RET 受体酪氨酸激酶 RetA 的功能。

Tonabersat (SB-220453,托那博沙) 是一种新型和可口服的的gap-junction 调节剂和CSD（Cortical spreading depression）抑制剂, 调节三叉神经节神经细胞和胶质细胞之间的细胞通讯并抑制神经源性炎症，用于治疗偏头痛和癫痫。

Troriluzole 是一种具有口服活性谷氨酸调节剂，具有抗癌活性。Troriluzole 可提高位于神经胶质细胞的兴奋性氨基酸转运体的表达，可用于研究脊髓小脑性共济失调、阿尔茨海默病和广泛性焦虑症 (GAD) 。

JBPOS0101 在阿尔茨海默病模型中调控淀粉样β蛋白、tau蛋白和胶质细胞。

inhibitor of both glial and neuronal uptake of glutamate, aspartate and cysteate.

glial glutamate transporter EAAT1 and EAAT2 inhibitor

TT-301 is a cytokine inhibitor and glial cell inhibitor.

TRC051384 HCl 是热休克蛋白 Hsp70 的诱导剂，可激活热休克因子-1 并增强神经元和神经胶质细胞中 Hsp72 的表达。

Ganglioside GQ1b is a tetrasialoganglioside that contains two sialic acid residues linked to an inner galactose unit. It stimulates phosphorylation of several ecto-type protein kinase substrates on the surface of GOTO human neuroblastoma cells when used at a concentration of 5 nM. Ganglioside GQ1b promotes differentiation of murine embryonic stem cells (mESCs) to neuronal precursor and glial cells via activation of the ERK1/2 pathway. It also induces differentiation of murine keratinocytes through phosphoinositide turnover. Ganglioside GQ1b mixture contains ganglioside GQ1b molecular species with C18:1 and C20:1 sphingoid backbones.

Apoptolidin is an apoptosis inducer originally isolated from Nocardiopsis bacteria. It inhibits the mitochondrial F1FO ATPase (Ki = 4-5 μM). Apoptolidin selectively kills transformed glial cells without significantly affecting untransformed cells. It also has antibiotic and antifungal actions.

Ceramide phosphoethanolamine (CPE) is an analog of sphingomyelin that contains ethanolamine rather than choline as the head group. It is the principal membrane phospholipid in invertebrates such as Drosophila, which lacks sphingomyelin. It is only produced in small amounts in mammalian cells, accounting for approximately 0.02 mol% of total phospholipids in mouse testis and brain. In Drosophila, CPE is biosynthesized by CPE synthase from ceramide and cytidine diphosphate-ethanolamine in the Golgi lumen. In mammals, it is biosynthesized by sphingomyelin synthase 2 (SMS2) in the plasma membrane and by sphingomyelin synthase-related protein (SMSr) in the endoplasmic reticulum (ER). In Drosophila, CPE has a role in glial ensheathment of axons. Disrupting CPE synthesis by depleting SMSr in vitro in mammalian cells leads to an accumulation of ER ceramides, which are then mislocalized to the mitochondria, inducing apoptosis. However, ceramide levels are not altered in transgenic mice lacking SMSr catalytic activity. CPEs (bovine) is a mixture of CPEs with variable N-acyl chain lengths.

Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing the human transporters). Reduced haloperidol (0.5 mg kg) increases latency to paw withdrawal in mouse models of capsaicin- but not force-induced mechanical hypersensitivity.

Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 |Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibitor. Bioorg.Med.Chem.Lett. 11 2007 PMID:11454468 |Williams et al (2003) Development of a scintillation proximity assay for analysis of Na+ Cl- -dependent neurotransmitter transporter activity. Anal. Biochem. 321 31 PMID:12963052

UDP-α-D-Glucose is an endogenous nucleotide sugar involved in glycosyltransferase reactions in metabolism. It has been shown to bind the P2Y14receptor (EC50= 0.35 μM), an atypical P2Y receptor involved in the activation of dendritic cells and glial cells.1It can also bind to and activate GPR17, inducing oligodendrocyte differentiation at a maximal concentration of 100 μM.2 1.Jacobson, K.A., Ivanov, A.A., de Castro, S., et al.Development of selective agonists and antagonists of P2Y receptorsPurinergic Signal.5(1)75-89(2009) 2.Lecca, D., Trincavelli, M.L., Gelosa, P., et al.The recently identified P2Y-like receptor GPR17 is a sensor of brain damage and a new target for brain repairPLoS One3(10)(2008)