traumatic brain injury

MTOB (α-keto-γ-Methylthiobutyric acid) is a substrate for c-terminal binding protein (CtBP) that interferes with the carcinogenic activity of CtBP in cell culture and mice. It also actively regulates TCF-4 signaling, leading to cancer stem cell (CSC) growth and self-renewal.

Enoxaparin sodium is a low-molecular-weight heparin (LMWH) that has recently been approved by the US FDA for use in patients with medically managed ST-segment myocardial infarction (STEMI), or STEMI with subsequent percutaneous coronary intervention (PCI)

Candesartan (CV 11974) is an angiotensin II receptor blocker widely used in the treatment of hypertension and heart failure.

Deferoxamine (Desferrioxamine B) is an iron chelator. Deferoxamine can be used to reduce the accumulation and deposition of iron in tissues. Deferoxamine can improve neurological dysfunction by inhibiting ferroptosis and neuroinflammation after traumatic brain injury. It has antioxidant, anti-proliferation and anti-tumor activities, and can induce the production of HIF-1α, apoptosis and autophagy in cancer cells. It can be used to treat acute iron toxicity and COVID-19 related diseases.

CHPG sodium salt is a selective agonist of mGluR5 that activates ERK and Akt signaling pathways and is utilized in studies on traumatic brain injury.

AMN082 is an mGluR7 agonist with antidepressant effects. AMN082 has a neuroprotective effect on neuronal apoptosis in rats with traumatic brain injury and attenuates cocaine- and morphine-induced locomotor sensitization and cross-sensitization in mice.

Repinotan HCl (Bay-x-3702) is an orally active, selective and potent 5-HT1A receptor agonist across the blood-brain barrier and is an aminomethylbenzidine derivative.Repinotan HCl has potent neuroprotective effects and can be used in studies of ischemic stroke and traumatic brain injury.

MW01-2-151SRM is a novel small molecule inhibitor of microglia activation that crosses the blood-brain barrier, has anti-neuroinflammatory effects, attenuates the up-regulation of glial cytokines in models of neuroinflammation, and can be used in studies of traumatic brain injury, Alzheimer's disease, and alginate toxicity.

Rabeximod is a potent immunomodulator that reduces the severity of autoimmune diseases in rat models. Rabeximod inhibits arthritis in a time-dependent manner by stimulating TLR2 and TLR4 downstream to block the activation of inflammatory cells, most likely macrophages. Rabeximod effectively reduces brain antigen presentation in mice during anti-inflammatory therapy for traumatic brain injury.

Repinotan (BAY x 3702 free base) is an orally active, selective 5-HT1A receptor agonist that crosses the blood-brain barrier (BBB), exhibits neuroprotective activity, counteracts morphine-induced depression of ventilation in anesthetized rats, and may be used in studies of acute ischemic stroke and traumatic brain injury.

Citicoline sodium (CDP-choline) is an endogenous intermediate in the synthesis of phosphatidylcholine. It also serves as a choline donor in the biosynthesis of the neurotransmitter acetylcholine. Citicoline sodium demonstrates protective effects in cerebral ischemia, traumatic brain injury, and memory disorders. Exogenous administration of citicoline to rodents (500 mg/kg i.p. immediately after ischemia and at 3-h reperfusion) has been shown to stimulate the synthesis of phosphatidylcholine, sphingomyelin, and cardiolipin and to attenuate the release of arachidonic acid and the accumulation of ceramide.

HEPPS exhibits inhibitory activity against the amyloid-beta precursor protein, reducing Aβ aggregation burden and improving neuronal autophagy flux, thereby alleviating neuronal apoptosis and traumatic brain injury (TBI) in mice. It can be used for research into Alzheimer's disease and neurological disorders.

Tetrahydroxystilbene-2-O-β-D-glucoside (EH-201) is a low MW inducer of erythropoietin. Tetrahydroxystilbene-2-O-β-D-glucoside induces expression of erythropoietin, PPAR-γ coactivator 1α (PGC-1α) and haemoglobin in astrocytes and PC12 neuronal-like cells. In vivo, Tetrahydroxystilbene-2-O-β-D-glucoside treatment restores memory impairment, as assessed by the passive avoidance test, in SD, Aβ and KA mouse models. In the hippocampus of mice given Tetrahydroxystilbene-2-O-β-D-glucoside in their diet, levels of erythropoietin, PGC-1α and haemoglobin were increased. Treatment with Tetrahydroxystilbene-2-O-β-D-glucoside might be a therapeutic strategy for memory impairment in neurodegenerative disease, physiological ageing or traumatic brain injury.

Anatibant is a potent non-peptide bradykinin B2 receptor antagonist. Anatibant reduces intracranial hypertension and histopathological damage after experimental traumatic brain injury.

CHPG is a selective mGluR5 agonist that reduces LDH release and neuronal apoptosis, activates the ERK and Akt pathways, and protects against traumatic brain injury. It also increases the number of differentiated human OPCs and alleviates LPS-induced inflammation.

Phenoxybenzamine is an α-1 adrenergic receptor antagonist. Phenoxybenzamine may exert a neuroprotective effect by reducing neuroinflammation after traumatic brain injury.

P7C3 is a class of neuroprotective aminopropyl carbazoles which has been shown to block neuronal cell death in models of neurodegeneration. It was shown that P7C3 molecules additionally preserve axonal integrity after injury, before neuronal cell death occurs, in a rodent model of blast-mediated traumatic brain injury (TBI). This protective quality may be linked to the ability of P7C3 molecules to activate nicotinamide phosphoribosyltransferase, the rate-limiting enzyme in nicotinamide adenine dinucleotide salvage.

Neuroprotective agent 12 is an orally active compound capable of crossing the blood-brain barrier, offering significant neuroprotective properties. It exhibits robust antioxidant and anti-inflammatory effects, markedly inhibiting cell death induced by glutamate and acrolein. This agent reduces the expression of PDE4B while elevating levels of HO-1, p-CREB, and BDNF. In a traumatic brain injury (TBI) mouse model, Neuroprotective agent 12 demonstrates potent neuroprotection and holds potential for research into TBI and other central nervous system disorders.

IRF1 antagonist 1 (8003-3282) is a potent antagonist of IRF1 (interferon regulatory factor), exhibiting anti-inflammatory properties. This compound helps maintain the integrity of the blood-brain barrier and reduces cerebral edema. Additionally, IRF1 antagonist 1 can enhance neurological outcomes in mouse models of acute traumatic brain injury (TBI).

EIDD-1723 is a progesterone analogue that binds to the progesterone receptor (PR) with an IC50 of 2.25 μM. As the prodrug of EIDD-036, EIDD-1723 may exert neuroprotective effects not only through the PR-dependent pathways but also via nongenomic mechanisms, such as regulating inflammation and oxidative stress. It is applicable in traumatic brain injury (TBI) research.

EIDD-036 is a C-20 oxime of Progesterone capable of crossing the blood-brain barrier and binding to progesterone receptors (PR) with an IC50 value of 171 nM. It is the active metabolite of EIDD-1723 and has poor water solubility, making rapid administration in acute injuries challenging. EIDD-036 is applicable for traumatic brain injury (TBI) research.

GPR17 agonist 2 (compound 10) is an agonist for the human GPR17 receptor. By functionally activating its target receptor, GPR17 agonist 2 regulates intracellular cAMP levels. It is useful for research related to multiple sclerosis, cerebral ischemia, traumatic brain injury, and spinal cord injury.

Indomethacin sodium hydrate is an effective orally active, competitive, and reversible inhibitor of COX-1 and COX-2, with IC50 values of 18 nM and 26 nM, respectively. It possesses anti-inflammatory, anticancer, and antimicrobial activities and is commonly used in research related to cancer, inflammation, and viral infections. Additionally, it can induce migraines and gastrointestinal injury and is used to study increased intracranial pressure secondary to severe traumatic brain injury in adults, as well as rheumatoid arthritis. It can also be used to induce gastric ulcer models.

SCH79797 is a potent and specific protease-activated receptor 1 (PAR1) antagonist with an IC50=70 nM with antimicrobial, anticancer, anti-inflammatory, and neuroprotective effects that attenuates thrombin-induced increase in CH25H expression in astrocytes, inhibits peritoneal dissemination of gastric cancer, and attenuates repetitive traumatic brain injury.