cortical cells

PRE-084 hydrochloride 是 σ1 的选择性激动剂在sigma 受体检测中，IC50值为44 nM。

3-MATIDA 是一种有效的 mGluR-1 拮抗剂（IC50：6.3 μM，大鼠 mGluR-1a）。显示出 ≥ 40 倍于其他受体的选择性：mGluR-5、mGluR-2、mGluR-4 (mGluR-4a) (IC50 > 300 μM)、NMDA 和 GluR (AMPA) (IC50 = 250 μM)。 3-MATIDA 在体外培养的鼠皮质细胞和大鼠海马切片培养物中充当神经保护剂。

Sciadopitysin 是一种双黄酮类化合物，来自银杏叶片中。它通过抑制NF-κB 活化并降低c-Fos 和NFATc1的表达来抑制 RANKL 诱导的破骨细胞生成和骨丢失。

SR 57227 hydrochloride(SR 57227A ) 是一种有效的、具有口服活性和选择性的 5-HT3 受体激动剂，具有穿越血脑屏障的能力和抗抑郁作用。它对大鼠皮质膜和整个 NG 108-15 细胞或其膜上的 5-HT3 受体结合位点的亲和力，IC50在 2.8 至 250 nM 之间。

Hypidone hydrochloride (YL0919) 是一种新型抗抑郁候选药物，具有作为 5-HT1A 受体激动剂和选择性 5-羟色胺再摄取抑制剂的双重活性。

MSN-125 effectively inhibits Bax Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons protect primary neurons against glutamate excitotoxicity. MSN-125 is an effective Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochond

Sauristolactam inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation. Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus Chi

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。

SR 57227A is a highly selective of peripheral and central 5-HT3 receptors and an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells. It exhibits anti-depressant like effects in rats and decreased isolation-induced aggressive beh

(±)11(12)-EET is a fully racemic version of the R S enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes.[1][2][3[]A higher proportion of 11(R),12(S)-EET is produced by the CYP450 isoforms CYP2C23 and CYP2C24 while CYP2B2 produces a higher proportion of 11(S),12(R)-EET.[3]11(12)-EET has been shown, along with 8(9)-EET to play a role in the recovery of depleted calcium pools in cultured smooth muscle cells[4] It also inhibits basolateral 18-pS potassium channels in the renal cortical collecting duct when used at a concentration of 100 nM.[5]11(12)-EET (50 μg kg per day) increases adhesion of isolated peripheral blood leukocytes in a chamber coated with P-selectin and ICAM-1 but does not affect choroidal neovascularization size following laser photocoagulation[6] It also has anti-inflammatory, angiogenic, and cardioprotective properties[7]

RC574 is an inhibitor of ferroptosis and a derivative of the antioxidant and hypocholesterolemic agent probucol .1It inhibits glutamate-induced cell death in HT22 cells (IC50= 276.2 nM) and mouse primary cortical neurons when used at a concentration of 3 μM. RC574 (3 μM) increases glutathione peroxidase 1 (GPX1) levels and GPX activity, as well as inhibits glutamate-induced mitochondrial superoxide anion production, in HT22 cells. It completely inhibits ferroptosis induced by the GPX4 inhibitor RSL3 in HT22 cells when used at concentrations ranging from 62.5 to 1,000 nM. 1.Bueno, D.C., Canto, R.F.S., de Souza, V., et al.New probucol analogues inhibit ferroptosis, improve mitochondrial parameters, and induce glutathione peroxidase in HT22 cellsMol. Neurobiol.57(8)3273-3290(2020)

KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It reduces infarction volume and increases the latency to fall in an accelerating rotarod test in a mouse model of focal cerebral ischemia induced by transient distal middle cerebral artery occlusion (MCAO) when administered at a dose of 100 mg/kg immediately following occlusion and again at 50 mg/kg following reperfusion. KUS121 (50 mg/kg) inhibits thinning of the retinal outer nuclear layer and preserves visual function in an rd10 mouse model of retinitis pigmentosa.1 1.Ikeda, H.O., Sasaoka, N., Koike, M., et al.Novel VCP modulators mitigate major pathologies of rd10, a mouse model of retinitis pigmentosaSci. Rep.45970(2014) 2.Kinoshita, H., Maki, T., Yasuda, K., et al.KUS121, a valosin-containing protein modulator, attenuates ischemic stroke via preventing ATP depletionSci. Rep.9(1)11519(2019)

Rasagiline-13C3is intended for use as an internal standard for the quantification of rasagiline by GC- or LC-MS. Rasagiline is an inhibitor of monoamine oxidase B (MAO-B; IC50= 4.43 nM for the rat brain enzyme).1It is selective for MAO-B over MAO-A (IC50= 412 nM for the rat brain enzyme). It inhibits serum and NGF withdrawal-induced apoptosis of PC12 cells when used at concentrations ranging from 0.01 to 100 μM.2Rasagiline inhibits rat brain MAO-Bin vivo(ED50= 0.1 mg kg).1It reduces cerebral edema in a mouse model of traumatic brain injury.2Rasagiline (0.1 mg kg) reduces cortical and hippocampal levels of full-length and soluble amyloid precursor protein (APP) in rats and mice. It also reduces α-synuclein-induced substantia nigral neuron loss and improves motor dysfunction in a mouse model of Parkinson's disease.3Formulations containing rasagiline have been used in the treatment of Parkinson's disease. 1.Youdim, M.B.H., Gross, A., and Finberg, J.P.Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase BBrit. J. Pharmacol.132(2)500-506(2001) 2.Youdim, M.B.H., and Weinstock, M.Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R) aminoindan-5-YL)-ethyl methyl carbamate]Cell. Mol. Neurobiol.21(6)555-573(2001) 3.Kang, S.S., Ahn, E.H., Zhang, Z., et al.α-Synuclein stimulation of monoamine oxidase-B and legumain protease mediates the pathology of Parkinson's diseaseEMBO J.37(12)e98878(2018)

Amyloid-β (25-35) (Aβ (25-35)) is an 11-residue fragment of the Aβ protein that retains the physical and biological characteristics of the full length peptide. It forms fibrils that react to thioflavin T and Congo red and are organized in a cross-β arrangement of β-strands similar to Aβ (1-40) and Aβ (1-42) fibrils. Aggregated Aβ (25-35) decreases the viability of rat adrenal PC12 cells. It also decreases the viability of primary rat cortical neurons at concentrations ranging from 1 nM to 30 μM. In vivo, intracerebral injection of Aβ (25-35) (20 nmol) in rats induces lesions of neuronal and tissue loss. Aggregated Aβ (25-35) administered intracerebroventricularly to rats induces learning and memory impairments in the Y-maze, novel object recognition, and contextual fear conditioning tests.

Potent and selective β-secretase (BACE) inhibitor (IC50 values are 10.2 and 20.3 nM for human BACE2 and BACE1, respectively). Displays >5,000-fold selectivity for BACE over other proteases including cathepsin D, pepsin and renin. Inhibits Aβ1-40 and Aβ1-42 production in cells expressing mutated APP. Reduces hippocampal and cortical Aβ and sAPPβ levels in an Alzheimer's disease mouse model.

Praeruptorin C 是白花前胡中的一种主要成分，是钙拮抗剂，pD2′值为 5.7。

8-CPT-2'-O-Me-cAMP（250 µM；1 h）可引导 Rap1 激活，进而在视网膜色素上皮细胞中促进连接蛋白及皮质 F-肌动蛋白的聚集。

(2R,3S)-Emricasan ((2R,3S)-PF 03491390) 作为Emricasan的一个异构体，属于高效的口服不可逆pan-caspase抑制剂。该化合物能够有效抑制由Zika 病毒 (ZIKV) 诱导的caspase-3活性增强，并能够保护人类皮层神经祖细胞免受损害。

Paeonilactone B ((+)-Paeonilactone B) 是一种来自白芍的单萜类化合物，具有神经保护活性，抑制氧化应激，在大鼠皮质细胞在抑制 H2O2 诱导的神经毒性。

Paeonilactone C significantly protects primary cultures of rat cortical cells against H2O2-induced neurotoxicity.

Aristolactam BII exhibits antimicrobial and antiinflammatory activity, it shows significant activity towards DPPH radical scavenging and potent inhibitory effects against tyrosinase mushroom. Aristolactam BII also exerts its significant neuroprotective ef

Dasycarpol(9beta-Hydroxyfraxinellone) shows significant neuroprotective activity against glutamate-induced neurotoxicity in primary cultures of rat cortical cells at a concentration of 0.1 microM. Dasycarpol also shows moderate inhibitory activity on lung

Hinokiresinol is a novel inhibitor of LTB4 binding to the human neutrophils, it has antiallergic effect, it inhibits IgE-induced mouse passive cutaneous anaphylaxis reaction. Hinokiresinol (trans-hinokiresinol) and nyasol (cis-hinokiresinol) are estrogen

Traxillaside has significant neuroprotective activities against glutamate-induced toxicity in primary cultures of rat cortical cells .