neuropathy

Infliximab is a monoclonal antibody, a human-mouse chimeric monoclonal antibody that inhibits TNF-α and prevents TNF-α from interacting with TNFR1 and TNFR2. Infliximab can be used to treat Crohn's disease and rheumatoid arthritis.

Neoline is an active ingredient of A. venetum root (PA) that ameliorates oxaliplatin-induced peripheral neuropathy in mice.Neoline inhibits Nav1.7 voltage-gated sodium channel currents (VGSC). It can be used as a labeling compound to determine the quality of PA products used in the study of neuropathic pain.

PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50: 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50: 0.11-25 μM), L-typ

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.

ACY-1083 is a small molecule inhibitor, a highly selective HDAC6 inhibitor (IC50=3 nM), with 260-fold higher selectivity over other classes of HDAC isoforms. It is brain-penetrant and used for research on chemotherapy-induced peripheral neuropathy.

Dimiracetam (NT-11624) is an orally active anti-neuropathy compound that inhibits hypersensitivity and neurological alterations and may be used in the study of cognitive disorders, depression and neuropathic pain.

Egis-11150 is an anti-neuropathy compound with pro-cognitive effects.

Cyclazosin HCl is a subtype-selective α-adrenergic receptor antagonist that competitively antagonizes norepinephrine-induced α(1B)-adrenergic receptor contraction and can be used to study non-arteritic ischemic optic neuropathy and other neurological diseases.

Ebaresdax hydrochloride has analgesic activity and is used in the study of painful diabetic neuropathy caused by type I or type II diabetes.

Propoxur (Propoxure) is an insecticide used to control cockroaches, flies, mosquitoes, and lawn and turf insects. Acute (short-term) exposure of humans to propoxur by ingestion leads to cholinesterase inhibition of red blood cells, with mild cholinergic symptoms including blurred vision, nausea, vomiting, sweating, and tachycardia; however, the effects are transient. Chronic (long-term) inhalation exposure has resulted in depressed cholinesterase levels, headaches, vomiting, and nausea in humans. Chronic ingestion studies in animals have reported depressed cholinesterase levels, depressed body weight, effects to the liver and bladder, and a slight increase in neuropathy. No information is available on the reproductive, developmental, or carcinogenic effects of propoxur in humans. Mixed results are available from cancer studies of propoxur in animals. EPA has not classified propoxur for carcinogenicity.

Epalrestat (ONO2235), an aldose reductase inhibitor, is well tolerated in Long-term therapy. It can effectually ameliorate the associated symptoms of diabetic neuropathy and delay the progression of the disease, particularly in patients with limited microangiopathy and good glycemic control.

J-147 is an experimental drug with reported effects against both Alzheimer's disease and ageing in mouse models of accelerated aging. It is a curcumin derivative and a potent neurogenic and neuroprotective drug candidate initially developed for the treatment of neurodegenerative conditions associated with aging that impacts many pathways implicated in the pathogenesis of diabetic neuropathy.

Acetyl-L-carnitine hydrochloride (Acetyl L-carnitine hydrochloride) is a nutritional supplement composed of the hydrochloride salt form of the acetylated form of the endogenously produced L-carnitine, with potential neuroprotective, cognitive-enhancing, anti-depressive and immunomodulating activities. It may also relieve peripheral neuropathy induced by chemotherapy, diabetes or other diseases. In addition, acetyl-L-carnitine may modulate the immune response by increasing T-lymphocytes maturation and may downregulate pro-inflammatory cytokines in response to viruses, such as SARS-CoV-2. It may also disrupt the ACE2 signaling pathway and inhibit the production of reactive oxygen species (ROS).

6-Hydroxyflavanone, extracted from the leaves of Acorus calamus, exhibits anti-inflammatory and anti-neuropathic pain activity by targeting cyclooxygenase-2 (COX-2), 5-lipoxygenase (5-LOX), as well as opioid and GABA-A receptors. 6-Hydroxyflavanone has anti-injury sensory properties in a streptozotocin-induced diabetic neuropathy model. in a streptozotocin-induced diabetic neuropathy model with anti-injury sensory properties.

KLS-13019 is a highly effective and orally active GPR55 receptor antagonist, a cannabidiol (CBD)-derived neuroprotective agent that can reverse chemotherapy-induced peripheral neuropathy (CIPN) and is suitable for studying hepatic encephalopathy (HE).

Myriocin (Thermozymocidin), a metabolite derived from Myriococcum albomyces, is a serine-palmitoyltransferase (SPT) inhibitor with potential antitumour, anticancer, and antiparasitic activities.Myriocin inhibits tumour growth by regulating macrophage polarisation and function through the PI3K/Akt/mTOR pathway.Myriocin inhibits HCV infection and can be used in the study of neurological diseases. Myriocin inhibits HCV infection and can be used to study neuropathy and fungal infections.

Kv7.2/Kv7.3 agonist 1 (Compound 16) is an orally effective agonist for the KV7.2/7.3 channels (KV7.2/7.3 channel/KCNQ2/3) with an EC50 of 1.03 μM. This compound demonstrates analgesic effects in mouse models of chronic constriction injury (CCI) and Streptozotocin-induced diabetic peripheral neuropathy (DPNP), with ED50 values of 12.02 mg/kg and 9.63 mg/kg, respectively.

SARM1-IN-4 (Compound 7) is an orally active SARM1 inhibitor that reduces plasma neurofilament light chain (NfL) levels in a mouse model following a 50 mg/kg oral dose. By inhibiting the NAD+ hydrolase activity of SARM1, it prevents programmed axon degeneration, making it useful for research in neurodegenerative and neurological diseases such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, and peripheral neuropathy.

ALR2-IN-6 (compound 9) is a potent competitive inhibitor of ALR2, with a Ki value of 0.064 μM. It is applicable in research related to neuropathy, retinopathy, and nephropathy.

Fluphenazine hydrochloride is an effective, orally active phenothiazine class dopamine receptor (dopamine receptor) antagonist. It blocks voltage-gated sodium ion channels (sodium channels) in neurons. The compound primarily exerts its effects by antagonizing postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular pathways. It counteracts stereotypy induced by methylphenidate in mice and suppresses climbing behavior. Fluphenazine hydrochloride is used in studying psychoses and diabetic-related painful peripheral neuropathy, with potential to inhibit SARS-CoV-2.

Mangafodipir is a hepatocyte-specific contrast agent and an effective inhibitor of conditions caused by CIPN (chemotherapy-induced peripheral neuropathy) and other oxidative stress pathways. It does not negatively impact the tumor-killing efficacy of chemotherapy.

Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active activator of Kv7.2/Kv7.3 channels and the TSPO. It activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). This compound protects motor neurons from degeneration caused by exposure to astrocyte-conditioned media from mice and humans with amyotrophic lateral sclerosis/frontotemporal dementia. Additionally, Kv7.2/Kv7.3 activator-3 stimulates axonal growth in dorsal root ganglia through TSPO and Kv7.2/3 activation and exhibits anticonvulsant effects in epilepsy models. It alleviates hyperalgesia in diabetic neuropathy patients, enhances the survival and regeneration of neurons after cervical neuropathy in rats, and accelerates the recovery of normal function in sensory and motor neurons.

COX-2-IN-57 is an orally active COX-2 inhibitor with an IC50 value of 0.02 μM. In a rat model with neuropathy induced by Cisplatin/radiation, it reduces MyD88 expression and lowers serum levels of COX-2, PGE2, and COX-1. COX-2-IN-57 demonstrates excellent analgesic effects in hot plate, cold allodynia, and Randall-Selitto tests, and provides liver/kidney protection. It is applicable for inflammation research.

Enprofylline (Enprofilina), a bronchodilator, acts primarily as a competitive nonselective phosphodiesterase inhibitor. Enprofylline is used in asthma, chronic obstructive pulmonary disease, and in the management of sickle cell disease, diabetic neuropathy, and cerebrovascular insufficiency.