neurotoxicity

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of iron death. Ferrostatin-1 potently inhibits Erastin-induced iron death in HT-1080 cells with an EC50 of 60 nM. Ferrostatin-1 also exhibits antioxidant and antifungal activities.

Oxidopamine hydrobromide (6-OHDA hydrobromide) is a neurotransmitter dopamine antagonist.

Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is an neurotransmitter dopamine antagonist.

Erbulozole (R 55104) is a potent synthetic microtubule inhibitor with anti-invasive, anti-tumor, and radiosensitizing activities that induces Wernicke's encephalopathy-like neurotoxicity.

S1R agonist 2 is a selective S1R agonist with a Ki of 88 nM for S2R and 1.1 nM for S1R and is protective against ROS and NMDA-induced neurotoxicity.

Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner, producing an IC of 0.85 μM in HEK cells.Orphenadrine is an antagonist of central and peripheral muscarinic receptors. Attenuation is blocked by mutations in pore residues Y652 or F656. Orphenadrine has antispasmodic, analgesic, and anticholinergic activity and protects against glutamatergic neurotoxicity in vitro and in vivo.Orphenadrine has inhibitory effects on sodium channels and can be used in the treatment of Parkinson's disease.

DB04760 is a highly selective, non-zinc-chelating inhibitor of MMP-13 (IC50: 8 nM). DB04760 obviously decreases paclitaxel neurotoxicity and has anticancer activity.

Copper histidine inhibited Ctr1-mediated cellular uptake of oxaliplatin in vitro without altering oxaliplatin accumulation of platinum or neurotoxicity in DRG tissues in vivo. Copper histidine is administered orally for the treatment of Menkes disease.

Benzamide (Amid kyseliny benzoove), an inhibitor of poly(ADP-ribose) polymerase, is a derivative of benzoic acid.

1-Aminocyclopropane-1-carboxylic acid (ACC) is an intermediate in the synthesis of ethylene, the plant hormone responsible for biological processes ranging from seed germination to organ senescence. It is a small molecule agonist at the glycine modulatory site of the NMDA receptor (EC50 = 0.7-0.9 μM) in the presence of low levels (1 μM) of glutamate and as a competitive antagonist at the glutamate-binding site on NMDA receptors (EC50 = 81.6 nM) with high levels (10 μM) of glutamate.2 This compound has been reported to protect against neuron cell death in vivo models of ischemia by enabling moderate levels of NMDA receptor activation and attenuating any excess NMDA receptor signaling that may lead to neurotoxicity.

Tetrahydropapaverine hydrochloride (Norlaudanosine HCl) , an analogue of salsolinol and tetrahydropapaveroline, has neurotoxicity on dopamine neurons.

Idebenone (CV-2619) is a synthetic analogue of ubiquinone (Coenzyme Q10), a vital cell antioxidant and essential component of the Electron Transport Chain (ETC).

1. Linarin (Acacetin-7-O-rutinoside) (acacetin-7-O-β-d-rutinoside) shows selective dose dependent inhibitory effect on acetylcholinesterase. 2. Linarin alleviates GalN LPS-induced liver injury by suppressing TNF-α-mediated apoptotic pathways. 3. Linarin prevents A beta-induced neurotoxicity through the activation of PI3K Akt, which subsequently inhibits GSK-3b and up-regulates Bcl-2. 4. The piperine significantly enhanced the oral absorption of Linarin in rats by inhibiting P-glycoprotein mediated cellular efflux during the intestinal absorption and likely simultaneously by inhibiting the metabolism of Linarin.

AM 281, a cannabinoid antagonist, reduces neurologic dysfunction and mortality rate after cecal ligation and puncture in rats.

PQM130 is a neuroprotective compound ,and is a potential anti-AD drug.

AG-825(Tyrphostin C15) is a selective and competitive ErbB2 inhibitor that inhibits tyrosine phosphorylation with an IC50 value of 0.35 μM.AG-825 (Tyrphostin C15) inhibits HER2 and shows anticancer activity in a mouse xenograft model of breast cancer.AG-825 ( Tyrphostin C15) is a potentially active molecule for overcoming manganese-induced neurotoxicity or the development of Alzheimer's disease, and promotes apoptosis in human neutrophils, which could be used in the study of breast cancer.

Setosusin is a meroterpenoid fungal metabolite originally isolated from C. setosus. It reduces neurotoxicity induced by amyloid-β (Aβ) aggregates in PC12 cells (EC50 = 112.6 μM). In vivo, setosusin (30 mg/kg) induces tremors in mice.

(+)-Afzelechin (Afzelechin) is isolated from Eysenhardtia subcoriacea. It is an α-glucosidase activity inhibitor, offering neuroprotective effects against glutamate-induced neurotoxicity in HT22 cells and improving reduced glutathione levels in rat pancreas homogenates.

Peimisine 3-O-β-D-glucopyranoside is a steroidal alkaloid isolated from the bulb of Monocarpus monocarpus with partial neuroprotective activity, and can be used for the study of rotenone-induced neurotoxicity in the PC12 cell line.

BML-259 is an inhibitor of CDK5 and CDK2 with IC50s of 64 and 98 nM, respectively. BML-259 can be used in studies about the treatment of cancer and neurodegenerative diseases.

Neuronotoxicity-IN-1 is a pyridothiazine derivative. Neuronotoxicity-IN-1 is an inhibitor of kainic acid neurotoxicity with neuroprotective activity[1].

HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated inhibitor of HDAC6 (IC50 = 0.025 μM) that inhibits Aβ 1-42 self-aggregation and AChE with IC50 values of 3.0 and 0.72 μM, respectively. Additionally, HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity.

HDAC6-IN-6 (compound 6a) is a potent HDAC6 inhibitor with an IC50 value of 0.025 μM that can penetrate the BBB. It exhibits strong inhibitory activity against AChE and Aβ 1-42 self-aggregation with IC50 values of 0.72 and 3.0 μM, respectively. HDAC6-IN-6 also enhances neurite outgrowth without significant neurotoxicity [1].

D-Arabitol is a polyol that can lead to neurotoxicity when accumulated in the body.