ischemic stroke

CHIR 98024 is a potent GSK-3α/β inhibitor with IC50 of 0.65 nM/0.58 nM in cell-free assays, with the ability to distinguish GSK-3 from its closest homologs Cdc2 and ERK2.

TRC051384 is a heat shock protein 70 (HSP70) inducer that reduces stroke-associated neuronal damage and increases survival in a rat model of transient ischemic stroke, activates heat shock factor-1 and leads to elevated molecular chaperone and anti-inflammatory activity, and enhances Hsp72 expression in neurons and glial cells.

Nelonemdaz (Neu2000) is an NMDA receptor antagonist with antioxidant activity and neuroprotective activity used in the study of cerebral infarction reperfusion injury and acute ischemic stroke.

Aptiganel (CNS-1102) is a non-competitive NMDA antagonist, a peptide that may be used to study acute ischemic stroke.

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.

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.

Pinokalant (LOE-908) is a novel non-selective cation channel inhibitor.Pinokalant significantly reduces cortical infarct volume in in vivo experiments, improves the metabolic and electrophysiological status of the ischemic penumbra region, and reduces the size of the lesion on magnetic resonance images in the acute phase after middle cerebral artery occlusion in rats.Pinokalant is a potential SARS-CoV-2 protease inhibitor for the study of stroke.

NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.

PF-03049423 is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of approximately 0.2 nM for rat and human thrombomodulin. PF-03049423 can be used in studies about acute ischemic stroke studies.

Cinepazide maleate (MD-67350), a maleate salt form of cinepazide, is a vasodilator.

Gambogic amide is a potent and selective agonist of tropomyosin receptor kinase A (TrkA) that promotes tyrosine phosphorylation and activates downstream signaling pathways including Akt and MAPK. Gambogic amide specifically binds to the cytoplasmic juxtamembrane domain of the TrkA receptor, thereby stimulating receptor dimerization and activation. Gambogic amide has been reported to prevent glutamate-induced neuronal cell death and demonstrates enhanced activity in a transient middle cerebral artery occlusion model of stroke. These biological properties support the utilization of Gambogic amide in research focused on neurodegenerative disorders, neuronal survival mechanisms, neurotrophic signaling pathways, and ischemic brain injury.

The quinuclidine PHA 568487 free base is an agonist of the alpha 7 nicotinic acetylcholine receptor that was designed to mitigate the bioactivation associated with the core scaffold and subsequently remove associated liabilities with in vivo tolerability.

FCPR03 is a selective inhibitor of phosphodiesterase 4 (PDE4) with IC50s of 31 nM, 47 nM, and 60 nM for PDE4B1, PDE4D7, and PDE4 catalytic domain, respectively. FCPR03 has neuroprotective, anti-inflammatory, and antidepressant-like effects.

IC87201 is a nNOS-PDZ/PSD-95-PDZ inhibitor. IC87201 showed great promise in cellular experiments and animal models of ischemic stroke and pain.

Tat-NR2B9c (NA-1) is a postsynaptic density-95 (PSD-95) inhibitor with neuroprotective and antiepileptic effects.Tat-NR2B9c inhibits PSD-95d2, PSD-95d1, and PSD-95, which prevents the activation of NMDA-induced NADPH oxidase in neurons, thereby blocking the production of superoxide, which reduces ischemic injury in the acute phase after stroke.

OBA-09 (2-oxopropanoyloxy benzoic acid) is a novel multimodal neuroprotectant synthesized as a hybrid of salicylic acid and pyruvate. Designed to synergize the anti-inflammatory properties of salicylic acid with the metabolic support and antioxidant capacity of pyruvate, OBA-09 combats ischemic brain injury effectively. It exhibits potent radical scavenging activity against superoxide, hydroxyl radicals, and hydrogen peroxide. Furthermore, it attenuates post-ischemic inflammation by inhibiting the NF-kB signaling pathway and the release of HMGB1. In stroke models, OBA-09 significantly reduces infarct volume and improves neurological scores.

ZD-1611 is an effective and selective ETA receptor antagonist. It is used for the research of ischemic stroke.

Annaosanchun (YC-6) is potentially for the treatment of acute ischemic stroke (AIS).

GABA-A Receptor Ligand-1 (Compound 4) is a ligand for the GABA-A receptor with a pKi of 7.27. It alleviates mitochondrial dysfunction, promotes neurite outgrowth and neuronal regeneration, and demonstrates neuroprotective effects in a rat ischemic stroke model.

HZS60 is a brain-penetrant NMDAR/TRPM4 inhibitor that shows promise in ameliorating cerebral ischemia. It provides significant neuroprotection against ischemic injury in primary neurons caused by NMDA and oxygen-glucose deprivation/reoxygenation. HZS60 demonstrates favorable pharmacokinetic properties and can inhibit cerebral ischemia-reperfusion injury, positioning it as a potential inhibitor for ischemic stroke.

TREK inhibitor-3 (Cpd8l) is a selective inhibitor of TREK-1 that can cross the blood-brain barrier, with an IC50 of 0.81 μM. It offers neuroprotective effects by significantly reducing cortical neuron death induced by oxygen-glucose deprivation/reoxygenation (OGD/R) and alleviating brain injury in middle cerebral artery occlusion/reperfusion (MCAO/R) model mice. TREK inhibitor-3 is utilized in ischemic stroke research.

Nrf2 activator 19 is a compound capable of crossing the blood-brain barrier and acts as an NRF2/HO-1 activator, offering potent antioxidant and neuroprotective effects. It effectively reduces brain damage and minimizes the accumulation of Reactive Oxygen Species (ROS). Additionally, Nrf2 activator 19 inhibits neuronal apoptosis, aiding in the recovery of neural function and motor skills. It has demonstrated significant potential in ischemic stroke research.

DB-10 serves as a precursor to 3-nbutylphthalide (NBP). It is absorbed by cells in a temperature and energy-dependent manner through the pyrilamine cation transporter. DB-10 enhances cell survival and rapidly converts into an active form in vivo, increasing accumulation within the brain. This compound is applicable in ischemic stroke research.

Neuroprotective agent 8 (compound AA-9) is an orally active neuroprotective agent that functions through antioxidant stress reduction and anti-inflammatory mechanisms. In a rat model of MCAO ischemic stroke, it activates PGC-1α and inhibits the NLRP3 inflammasome.