glial

TRC051384 is a heat shock protein 70 (HSP70) inducer that reduces stroke-associated neuronal damage and increases survival in a rat model of transient ischemic stroke, activates heat shock factor-1 and leads to elevated molecular chaperone and anti-inflammatory activity, and enhances Hsp72 expression in neurons and glial cells.

MW01-2-151SRM is a novel small molecule inhibitor of microglia activation that crosses the blood-brain barrier, has anti-neuroinflammatory effects, attenuates the up-regulation of glial cytokines in models of neuroinflammation, and can be used in studies of traumatic brain injury, Alzheimer's disease, and alginate toxicity.

1. Methyl eugenol (4-allylveratrole) is a natural constituent of the essential oils of a number of plants widely used in foodstuffs as flavouring agents, in view of the carcinogenic potential of ME, the need to check its presence in food products with effective analytical methods. 2. Methyleugenol has insecticidal properties. 3. Methyleugenol can inhibit the production of nitric oxide and decreased the protein expression of inducible nitric oxide synthase, it down-regulates the production of pro-inflammatory cytokines in the ischemic brain as well as in immunostimulated mixed glial cells; indicates that methyleugenol could be useful for the treatment of ischemia inflammation-related diseases. 4. Methyleugenol has cytotoxicity and genotoxicity. 5. Intravenous (i.v.) treatment with methyleugenol (ME) in either anesthetized or conscious rats elicits hypotension, an effect that seems related to an active vascular relaxation rather than withdrawal of sympathetic tone. 6. Methyleugenol has antinociceptive effect on the second phase of formalin-induced pain, may be due to the inhibition of N-methyl-d-aspartic acid (NMDA) receptor-mediated hyperalgesia via GABA(A) receptors. 7. Methyleugenol has elaxant and antispasmodic actions on guinea-pig isolated ileum.

O-PHOSPHO-L-SERINE is an ester of serine and phosphate, which are normal metabolites in human biofluids.O-phospho-L-serine is a phagocytosis inhibitor that inhibits glial cell proliferation and cone cell regeneration after photodamage.

TGN-020 is an inhibitor of Aquaporin 4 (AQP4, IC50: 3.1 μM), the most abundant water channel in the brain.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

TRC051384 is an inducer of heat shock protein Hsp70, activating heat shock factor-1 and enhancing Hsp72 expression in neurons and glial cells.

BT-13 is a selective agonist of glial cell line-derived neurotrophic factor (GDNF) receptor RET independently of GFLs. BT-13 promotes neurite growth from sensory neurons in vitro.

BT18 is a mimic with function similar to glial cell line-derived neurotrophic factor (GDNF). BT18 has an effect on RET receptor tyrosine kinase RetA and GDNF family receptor GFRα1 function.

Tonabersat (SB-220453) is a novel and orally available gap-junction modulator and CSD (Cortical spreading depression) inhibitor that regulates cellular communication between trigeminal ganglion neuronal cells and glial cells and inhibits neurogenic inflammation for the treatment of migraine and epilepsy.

Troriluzole is an orally active glutamate modulator with anticancer activity.Troriluzole enhances the expression of excitatory amino acid transporters located in glial cells and is used in the study of spinocerebellar ataxia, Alzheimer's disease, and generalized anxiety disorder (GAD).

JBPOS0101 modulates amyloid-beta protein, tau protein, and glial cells in Alzheimer's disease models.

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.

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)

PAQ is a neuroprotective agent. It protects dopaminergic neurons from cell death without inhibiting glial cell proliferation in a rat midbrain culture model of Parkinson's disease when used at a concentration of 10 μM. PAQ (25 or 50 mg/kg, twice per day) prevents loss of dopaminergic neurons in the substantia nigra in a mouse model of Parkinson's disease induced by MPTP.

MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a potent and selective inhibitor of p38α MAPK with a Ki value of 101 nM. It exhibits excellent CNS penetration and oral bioavailability, and effectively suppresses the phosphorylation of MK2, a substrate of endogenous p38α MAPK, in activated glial cells.

L-Cytidine, an L-configurational form of Cytidine, is a pyrimidine nucleoside and a component of RNA. It influences the glial glutamate cycle, brain phospholipid metabolism, catecholamine synthesis, and mitochondrial function [1] [2].