neurotoxicity

Oxidopamine hydrobromide (6-OHDA hydrobromide) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the pro-inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

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.

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

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

Oxidopamine hydrochloride (6-Hydroxydopamine hydrochloride) is a widely used neurotoxin and an antagonist of the neurotransmitter dopamine. It selectively destroys dopaminergic neurons, promotes COX-2 activation, induces PGE2 synthesis, and stimulates the secretion of the inflammatory cytokine IL-1β. It is commonly used to establish animal models of Parkinson’s disease (PD).

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

Tolmetin (Tolectin) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of tolmetin is as a Cyclooxygenase Inhibitor. The chemical classification of tolmetin is Nonsteroidal Anti-inflammatory Compounds.

1. Talatisamine (12 μM) and TEA (5mM) inhibits the enhanced I(K) caused by Aβ4 oligomers, attenuates cytotoxicity of Aβ oligomers by restoring cell viability and suppressing K(+) loss related apoptotic response. 2. Talatisamine can therefore be considered

Hibifolin is a flavonol glycoside natural product,is a potential inhibitor of adenosine deaminase (Ki of 49.92 μM). Hibifolin protects neurons against beta-amyloid-induced neurotoxicity.

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.

4-Hydroxyestrone, an endogenous estrogen metabolite, can strongly protect neuronal cells against oxidative damage.

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

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

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.

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.

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.

Capsaicin is an active natural component found in chili peppers and acts as a TRPV1 agonist (EC50 = 0.29 μM). It possesses multiple activities, including pain relief, antitumor, anti-inflammatory, antioxidant, and neuroprotective effects, as well as some neurotoxicity. Capsaicin can be used to establish itch models.

Spermine (Neuridine) is an endogenous polyamine in the human body. As a direct free radical scavenger, it exhibits antiviral activity and protects DNA from free radical damage; it is also a key regulator of cell proliferation, differentiation, and apoptosis. Spermine inhibits certain bacteria, particularly strains of Staphylococcus aureus. Spermine induces striatal neurotoxicity in a dose-dependent manner. Spermine reversibly inhibits DNA synthesis, mixed lymphocyte reactions, and the induction of cytolytic lymphocyte reactions in primary cultures of mouse splenocytes.

Fenobucarb is a broad-spectrum carbamate insecticide and AChE inhibitor primarily used to control various flukes damaging crops. It exhibits neurotoxicity to zebrafish foetal development and induces muscle spasms and paralysis in insects, fish, and mammals.

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.

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

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

Indole-2-carboxylic acid is an indole carboxylic acid compound with multi-target biological activity, exhibiting neuroprotective, antiviral, and antioxidant properties. Indole-2-carboxylic acid is a competitive antagonist at the glycine site of the NMDA receptor (Ki = 15 μM). Indole-2-carboxylic acid specifically inhibits the potentiating effect of glycine on NMDA-gated currents, blocking the neurotoxicity caused by excessive NMDA receptor activation, and can be used in research on the treatment of neurodegenerative diseases and cerebral ischemic injury. Indole-2-carboxylic acid is also an HIV-1 integrase inhibitor; it interferes with the integration of viral DNA into the host genome and can be used in the development of anti-HIV drugs.

Cefepime (BMY-28142) is a cephalosporin antibiotic with antimicrobial activity, induces neurotoxicity, inhibits both Gram-positive and Gram-negative, and can be used in the study of anaerobic bacteria.