plasticity

Cardiogenol C hydrochloride (Cardiogenol C) 是一种细胞渗透性嘧啶诱导剂，能够促使 ESCs 分化为心肌细胞。在有限的可塑性范围内，它可以对已经沿袭的祖细胞类型产生心肌生成效应，是一种心肌生成试剂，在动物模型中可以用作细胞移植研究中提高心脏修复的工具。

Rhosin hydrochloride 是一种特异性 RhoA 亚家族Rho GTPases 抑制剂，抑制 RhoA-GEF 相互作用。Rhosin hydrochloride可显著诱导细胞凋亡，不影响细胞周期进程。[1]

Cardiogenol C 是一种细胞渗透性嘧啶诱导剂，能够诱导 ESCs 分化为心肌细胞(EC50:100 nM)。在有限的可塑性范围内，它可以对已经沿袭的祖细胞类型产生心肌病，是一种心肌发生剂。

ZD7288 (ICI D7288) 是一种选择性超极化激活的环核苷酸门控通道阻滞剂，可抑制海马突触可塑性。

Cutamesine dihydrochloride (SA4503 dihydrochloride) 是一种选择性 σ1 受体激动剂，IC50值为 17.4 nM。

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy[1]. Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons[1]. Afizagabar (1 and 3 mg kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine[1]. [1]. Etherington LA, et al. Selective inhibition of extra-synaptic α5-GABAA receptors by S44819, a new therapeutic agent. Neuropharmacology. 2017;125:353-364.

Ganglioside GM1is a monosialylated ganglioside and the prototypic ganglioside for those containing one sialic acid residue.1,2It is found in a large variety of cells, including immune cells and neurons, and is enriched in lipid rafts in the cell membrane.3It associates with growth factor receptors, including TrkA, TrkB, and the GDNF receptor complex containing Ret and GFRα, and is required for TrkA expression on the cell surface. Ganglioside GM1interacts with other proteins to increase calcium influx, affecting various calcium-dependent processes, including inducing neuronal outgrowth during differentiation. Ganglioside GM1acts as a receptor for cholera toxin, which binds to its oligosaccharide group, facilitating toxin cell entry into epithelial cells of the jejunum.4,5Similarly, it is bound by the heat-labile enterotoxin fromE. coliin the pathogenesis of traveler's diarrhea.6Ganglioside GM1gangliosidosis, characterized by a deficiency in GM1-β-galactosidase, the enzyme that degrades ganglioside GM1, leads to accumulation of the gangliosides GM1and GA1in neurons and can be fatal in infants.1Levels of ganglioside GM1are decreased in the substantia nigra pars compacta in postmortem brain from patients with Parkinson's disease.3Ganglioside GM1mixture contains a mixture of ovine ganglioside GM1molecular species with primarily C18:0 fatty acyl chain lengths, among various others. [Matreya, LLC. Catalog No. 1544] 1.Kolter, T.Ganglioside biochemistryISRN Biochem.506160(2012) 2.Mocchetti, I.Exogenous gangliosides, neuronal plasticity and repair, and the neurotrophinsCell Mol. Life Sci.62(19-20)2283-2294(2005) 3.Ledeen, R.W., and Wu, G.The multi-tasked life of GM1 ganglioside, a true factotum of natureTrends Biochem. Sci.40(7)407-418(2015) 4.Turnbull, W.B., Precious, B.L., and Homans, S.W.Dissecting the cholera toxin-ganglioside GM1 interaction by isothermal titration calorimetryJ. Am. Chem. Soc.126(4)1047-1054(2004) 5.Blank, N., Schiller, M., Krienke, S., et al.Cholera toxin binds to lipid rafts but has a limited specificity for ganglioside GM1Immunol. Cell Biol.85(5)378-382(2007) 6.Minke, W.E., Roach, C., Hol, W.G., et al.Structure-based exploration of the ganglioside GM1 binding sites of Escherichia coli heat-labile enterotoxin and cholera toxin for the discovery of receptor antagonistsBiochemistry38(18)5684-5692(1999)

Highly potent and selective group II metabotropic glutamate receptor antagonist. Disodium salt of LY 341495 Fitzjohn et al (1998) The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology 37 1445 PMID:9886667 |Ornstein et al (1998) 2-Substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl) glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioav J.Med.Chem. 41 358 PMID:9464367 |Johnson et al (1999) [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells. Neuropharmacology 38 1519 PMID:10530814

NVS-BET-1 是 BET 溴结构域抑制剂。NVS-BET-1可以调节角质形成细胞可塑性。

AMPA-IN-1 是一种 AMPA 受体的有效抑制剂。AMPA 受体是一种在大脑中广泛表达的受体，在调节快速兴奋性突触传递和突触可塑性中具有核心作用。AMPA-IN-1 对包括癫痫在内的多种中枢疾病具有潜在的研究价值。

NCI-006 is a potent new inhibitor of lactate dehydrogenase (LDH) that disrupts tumor growth in mice. LDH inhibition slows tumor growth but rapidly redirects pyruvate to support mitochondrial metabolism. Inhibiting both mitochondrial complex 1 and LDH suppresses metabolic plasticity of glycolytic tumors in vivo, significantly prolonging tumor growth inhibition.

PDE1-IN-1can enhance levels of the second messengers cAMP cGMP leading to the expression of neuronal plasticity-related genes, neurotrophic factors, and neuroprotective molecules. These neuronal plasticity enhancement properties make PDE1 inhibitors good candidates as therapeutic agents in many neurological conditions.

Neurogranin (48-76)，mouse 为对应 Neurogranin 48-76 残基的多肽。该化合物是突触后表达的钙调素结合蛋白，通过调节 (Ca2+-CaM) 通路，介导 NMDAR 驱动的突触可塑性功能。

Leptin(116-130)是一种生物活性的瘦素片段，能促进AMPA受体运输至突触并加强活动依赖性的海马突触可塑性。此外，Leptin(116-130)在抗淀粉样蛋白毒性模型中有效阻止海马突触损伤和神经元细胞死亡，显示出对研究阿尔茨海默病(AD)具有重要潜力。

Gangliotetraose（Gg4）是一种含有GM1及其唾液酸化衍生物的四糖。它能促进分化神经元核内Ca2+的外流，进而降低核内Ca2+浓度。Gg4参与调节神经元的可塑性、修复过程以及大脑中神经营养素的释放。

CPF-7（Caerulein precursor fragment）是一种促进胰岛素释放的肽，可以通过增加PANC-1导管细胞中Snai1表达来引导上皮-间质转换（EMT），并且CPF-7还能通过提高Ngn3表达以诱导外分泌细胞可塑性。此外，CPF-7适用于2型糖尿病的相关研究。

DU-14 是一种有效的steroid sulfatase抑制剂，IC50为55.8 nM。DU-14 抑制MCF-7细胞增殖 (IC50 = 38.7 nM)。DU-14 对神经毒性Aβ具有神经保护作用，表明DU-14上调内源性DHEAS可能有助于减轻Aβ诱导的空间记忆和突触可塑性损伤。

Sp-8-pCPT-cGMPS 是一种对CNG通道具有高激活作用的化合物(cyclic guanosine monophosphate-gated channel)，并且作为 PKG (I α、I β 和 II 型) 以及 PKA II 型的疏水性活化剂显示出色的细胞膜穿透能力和对磷酸二酯酶的高稳定性。此外，Sp-8-pCPT-cGMPS 还常用于探究 cGMP 在神经可塑性及突触功能中的调控机制。

8-pCPT-cGMP-AM（8-(4-Chlorophenylthio)-cGMP-AM）作为PKG激动剂8-pCPT-cGMP的前体化合物，拥有较高的膜渗透性。此化合物可通过增强cGMP的膜透过性，进而在细胞内经由酯酶水解转变为其活性形式，激活PKG。研究人员常利用8-pCPT-cGMP-AM来研究cGMP信号在神经可塑性与记忆形成过程中的功能。

TAT-DEF-Elk-1 TFA is a cell-penetrating peptide Elk-1 inhibitor, mimics and specifically interferes with the DEF domain of Elk-1. TAT-DEF-Elk-1 blocks Elk-1 phosphorylation and prevents Elk-1 nuclear translocation without interfering with ERK nor MSK1 act

CMX-8933 是一种由8个氨基酸组成的肽段，源自金鱼脑神经营养因子的室管膜蛋白。该化合物能够提升c-Jun N-末端激酶 (JNK) 的活性，促进JNK和c-Jun蛋白的磷酸化，并增加c-Jun及c-Fos mRNA在细胞中的水平。CMX-8933 主要用于探索室管膜蛋白在神经可塑性、学习、记忆形成和神经再生中的功能。

Pep63 (VFQVRARTVA) 是一种具有神经保护功能的肽。它能促进突触可塑性及增强记忆力，并且可与 Aβ1-42 寡聚体进行竞争性结合，从而阻断 Aβ 纤维的形成。该化合物可用于阿尔茨海默病 (AD) 的相关研究。