stroke

Minocycline hydrochloride (Minocycline HCl) is a tetracycline antibiotic with excellent absorption and tissue penetration that is used for several bacterial infections as well as treatment of acne. Minocycline hydrochloride can cause both an acute hepatitis-like syndrome occurring within 1 to 3 months of starting therapy or a more insidious chronic hepatitis with autoimmune features typically after long-term treatment.

Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.

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.

Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long-chain fatty acid that inhibits fatty acid transport into cells. It is a potent and irreversible inhibitor of the mitochondrial respiratory chain and binds the CD36 receptor on the surface of microglia. Sulfosuccinimidyl oleate is neuroprotective and alleviates stroke-induced neuroinflammation [1] [2].

(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5-methylpyrimidin-2-yl)butane-2-sulfonamide is an Apelin receptor agonist with an EC50 for Apelin receptors of 0.012 µM.(2R,3S)-N-(4-(2,6-dimethoxyphenyl)-5-(5-methylpyridin-3-yl)-4H-1,2,4-triazol-3-yl)-3-(5- methylpyrimidin-2-yl)butane-2-sulfonamide is used in the treatment of heart failure, atherosclerosis, obesity, diabetes mellitus, amyotrophic lateral sclerosis, coronary artery disease, hypertension, stroke and myocardial infarction.

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.

TGX-115 is a cell-permeable and potent inhibitor of the PI 3-K isoform p110β p110δ (IC50 values of 0.13 μM for p110β and 0.63 μM for p110δ), an enzyme that regulates platelet adhesion and inhibits phosphoinositide (PI) 3-kinase, and can be used to treat coronary artery occlusion, stroke, acute coronary artery It can be used to treat cardiovascular diseases such as coronary occlusion, stroke, acute coronary syndrome, acute myocardial infarction, restenosis, atherosclerosis and unstable angina.

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

Lifarizine FA is a sodium channel blocker used in the treatment of neurological disorders and cardiovascular diseases, study of stroke.

ME-3221 is an angiotensin AT1 receptor antagonist that prevents hypertensive complications in aged stroke-prone hypertensive rats.

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.

Tirilazad mesylate (U 74006F) is a non-glucocorticoid, lipid peroxidation inhibitor with antiviral and neuroprotective activities. It confines intracellular intramembranous foci, attenuates spinal cord injuries induced by trauma, stroke, and ischemia reperfusion injuries, inhibits toxins in dogs, and is used in the study of neurological disorders.

Farnesyl Pyrophosphate ammonium (Farnesyl diphosphate ammonium) is a metabolic intermediate of the MVA pathway that acts as a newly identified danger signal to trigger acute cell death and induce neuronal loss in stroke.

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.

Azilsartan (TAK-536) is an Angiotensin 2 Receptor Blocker that acts as an Angiotensin 2 Type 1 Receptor Antagonist, leading to a physiologic effect of decreased blood pressure.

Hydralazine hydrochloride (Apresoline) is the hydrochloride salt of hydralazine, a phthalazine derivative with antihypertensive and potential antineoplastic activities. Hydralazine alters intracellular calcium release and interferes with smooth muscle cell calcium influx, resulting in arterial vasodilatation. This agent also inhibits the phosphorylation of myosin protein and chelation of trace metals required for smooth muscle contraction, resulting in an increase in heart rate, stroke volume, and cardiac output. In addition to its cardiovascular effects, hydralazine inhibits DNA methyltransferase, which may result in inhibition of DNA methylation in tumor cells.

Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.

Edoxaban (Lixiana) (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with K i s of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and is able to be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with K i s of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and is potential for thromboembolic diseases treatment [1] [2] [3].

4-POBN (Myeloperoxidase Inhibitor 1) is a potent and irreversible inhibitor of myeloperoxidase (IC50 = 0.3 µM). 4-POBN can be used in studies about subacute stroke.

sn-Glycero-3-phosphocholine (Choline glycerophosphate) is a natural choline compound found in the brain and in milk. It is also a parasympathomimetic acetylcholine precursor which may have a potential for the treatment of Alzheimer's disease and dementia. sn-Glycero-3-phosphocholine rapidly delivers choline to the brain across the blood–brain barrier and is a biosynthetic precursor of the acetylcholine neurotransmitter. It is a non-prescription drug in most countries due to its Generally Recognised As Safe (GRAS) status [1]. Studies have investigated its efficacy for cognitive disorders including stroke and Alzheimer's disease. An Italian multicentre clinical trial on 2, 044 patients suffering from recent stroke were supplied Glycerylphosphorylcholine in doses of 1, 000 mg day for 28 days and 400 mg three times per day for the five ensuing months. The trial confirmed the therapeutic role of alpha-GPC on the cognitive recovery of patients based on four measurement scales, three of which reached statistical significance [2].

Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.