brain function

PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.

Atomoxetine hydrochloride (LY 139603) is the hydrochloride salt of atomoxetine, a phenoxy-3-propylamine derivative and selective non-stimulant, norepinephrine reuptake inhibitor with cognitive-enhancing activity. Although its precise mechanism of action is unknown, atomoxetine appears to selectively inhibit the pre-synaptic norepinephrine transporter, resulting in inhibition of the presynaptic reabsorption of norepinephrine and prolongation of norepinephrine activity in the synaptic cleft. The effect on cognitive brain function may result in improved attention and decreased impulsivity and activity levels.

Pivagabine (CXB-722), a hydrophobic 4-aminobutyric acid derivative, exhibits neuromodulatory activity and successfully penetrates the blood-brain barrier in rats. It counteracts the impact of foot shock on GABAA receptor function and corticotropin-releasing factor (CRF) levels in the rat brain.

3-Hydroxybutyric acid (Butanoic acid) (or beta-hydroxybutyrate) is a ketone body. Like the other ketone bodies (acetoacetate and acetone), levels of 3-hydroxybutyrate in blood and urine are raised in ketosis. In humans, 3-hydroxybutyrate is synthesized in the liver from acetyl-CoA and can be used as an energy source by the brain when blood glucose is low. Blood levels of 3-hydroxybutyric acid levels may be monitored in diabetic patients to look for diabetic ketoacidosis. Persistent mild hyperketonemia is a common finding in newborns. Ketone bodies serve as an indispensable source of energy for extrahepatic tissues, especially the brain and lung of developing mammals. Another important function of ketone bodies is to provide acetoacetyl-CoA and acetyl-CoA for the synthesis of cholesterol, fatty acids, and complex lipids. During the early postnatal period, acetoacetate (AcAc) and beta-hydroxybutyrate are preferred over glucose as substrates for synthesis of phospholipids and sphingolipids in accord with requirements for brain growth and myelination. Thus, during the first 2 weeks of postnatal development, when the accumulation of cholesterol and phospholipids accelerates, the proportion of ketone bodies incorporated into these lipids increases. On the other hand, an increased proportion of ketone bodies is utilized for cerebroside synthesis during the period of active myelination. In the lung, AcAc serves better than glucose as a precursor for the synthesis of lung phospholipids. The synthesized lipids, particularly dipalmitoylphosphatidylcholine, are incorporated into surfactant, and thus have a potential role in supplying adequate surfactant lipids to maintain lung function during the early days of life (PMID: 3884391 ). 3-Hydroxybutyric acid is found to be associated with fumarase deficiency and medium-chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism.

CSF1R-IN-7 is a highly selective CSF-1R inhibitor with good brain penetration for the treatment of a variety of diseases associated with microglia-mediated neuroinflammation, particularly Alzheimer's disease and other neurodegenerative disorders.CSF-1R is a type III receptor tyrosine kinase that is expressed predominantly on microglia (immune cells in the brain) and regulates the development, survival and function of microglia.

1-(3,4-dihydroxyphenyl)-2-(dimethylamino)ethan-1-one hydrochloride is a cholinergic agent that inhibits choline metabolism, which leads to increased levels of acetylcholine in the brain, which in turn enhances cognitive function and memory.

TMPH is an inhibitor of nAChR and inhibits nAChRs lacking α5, α6, or β3 subunits. TMPH can be used in studies about nAChR dysfunction or neurological disorders.

SNT-207858 free base is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor(IC50 of 22 nM (binding) and 11 nM (function), on the MC-4 receptor).

SNT-207858 is a selective, blood brain barrier penetrating, potent and orally active antagonist of melanocortin-4 (MC-4) receptor. SNT207858 has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.

Pyrocatechol sulfate, a phenolic metabolite found in human plasma, is associated with the intake of specific foods such as berries and the state of the gut microbiome. It serves as a potential urinary biomarker for kidney function, dialysis clearance rates, whole grain consumption, and regular coffee intake. Additionally, in conjunction with other phenolic sulfates, pyrocatechol sulfate plays a role in regulating various biological functions, including those related to brain health and the rhythmic beating of cardiac cells.

TAC (TERT Activator Compound) acts as an activator of TERT, upregulating TERT transcription via the MEK ERK AP-1 cascade. It enhances telomere synthesis, reduces markers of aging, inflammation, and degeneration, and preserves brain function, underscoring TERT's potential in anti-aging and related diseases.

Cinoxopazide is recognized for its potential to enhance cognitive efficiency in healthy individuals, support brain function in the elderly, and address issues arising from attentiveness and or memory impairments. This compound is used to boost cognitive function, aiding in maintaining brain health for the elderly while also offering intellectual stimulation benefits for typical adults.

KNa1.1-IN-2 (Compound Z05) is a selective KNa1.1 channel inhibitor capable of penetrating the blood-brain barrier, and exhibits significant efficacy on hERG channels. It binds to KNa1.1 channels, effectively blocking channel activity caused by Gain-of-function (GOF) mutations, thus intervening in KCNT1-related seizures. Additionally, it inhibits the GOF mutant Y796H, making KNa1.1-IN-2 a promising candidate for research into KCNT1-associated epilepsy disorders.

N-Octanoyl dopamine surpasses dopamine in preserving the contractile function of donor hearts from brain-dead individuals. Additionally, N-Octanoyl dopamine inhibits cytokine production in activated T cells and reduces the expression of MHC-II and adhesion molecules in endothelial cells stimulated by IFNγ.

BuChE-IN-16 (Compound 6a) is an orally active, blood-brain barrier-permeable, and selective BuChE inhibitor with an IC50 of 0.33 μM. It exhibits anti-inflammatory and neuroprotective effects, improves cognitive function in Alzheimer's disease (AD) zebrafish models, and alleviates scopolamine-induced memory impairment in mice. BuChE-IN-16 is applicable for Alzheimer's disease research.

Q134R, a neuroprotective derivative of hydroxyquinoline, effectively inhibits nuclear factor of activated T-cell (NFAT) signaling and possesses the ability to cross the blood-brain barrier. This compound shows promise for research into Alzheimer's disease (AD) and aging-related disorders[1].

Cutamesine dihydrochloride (SA4503 dihydrochloride) is a selective σ1 receptor agonist (IC50: 17.4 nM). It shows selectivity for σ1 over σ2 receptors, and inhibits angiotensin II-induced cardiomyocyte hypertrophy in vitro and attenuates myocardial hypertrophy in vivo. In a rat model of experimental stroke, it enhances brain plasticity and sensorimotor function.

The metallo-protein Cu/Zn-superoxide dismutase (SOD1) is a ubiquitous enzyme responsible for scavenging superoxide radicals. Mutations in SOD1, which alter its metal binding capacity and can result in protein misfolding and aggregation, have been linked to familial amyotrophic lateral sclerosis (ALS). Cu-ATSM is an orally bioavailable, blood-brain barrier permeable complex that has traditionally been used in cellular imaging experiments to selectively label hypoxic tissue via its susceptibility to reduction by oxygen-depleted mitochondria. More recently, Cu-ATSM has been reported to improve locomotor function and survival in a transgenic ALS mouse model by delivering copper specifically to cells in the spinal cords of mice producing misfolded SOD1 proteins. Copper chaperone for SOD (CCS) is presumed to utilize the copper from Cu-ATSM to prevent misfolding of the SOD1 protein.

N-Acetyl lysyltyrosylcysteine amide is a non-toxic, potent, reversible, and specific myeloperoxidase (MPO) tripeptide inhibitor that effectively inhibits MPO production in vivo, attenuates neuronal damage, preserves brain tissue and neurological function post-stroke, and inhibits MPO-dependent hypochlorite (HOCl) production, protein nitration, and LDL oxidation. It is also used in the study of bronchial dysplasia.

Forsythoside B binds to LPS and reduces the biological activity of serum LPS, and inhibits NF-κB activation. Forsythoside B inhibits the inflammatory response and has antioxidant properties. Potent neuroprotective effects with a favorable therapeutic time

2-(4-methoxyphenyl)-2-oxoethyl 2-hydroxy-5-methylbenzoate is a pro-neurotropic drug used to enhance cognitive function by increasing the synthesis and release of acetylcholine in the brain as well as by inhibiting the breakdown of acetylcholine by acetylcholinesterase.

L-Cytidine, an L-configurational form of Cytidine, is a pyrimidine nucleoside and a component of RNA. It influences the glial glutamate cycle, brain phospholipid metabolism, catecholamine synthesis, and mitochondrial function [1] [2].

FPR2 agonist 2 is a potent FPR2 agonist with blood-brain barrier permeability that acts on h-FPR2 (EC50: 0.13 nM), inhibiting the production of pro-inflammatory cytokines, counteracting changes in mitochondrial function, and inhibiting caspase-3 activity.

NXPZ-2 is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor (Ki: 95 nM, EC50: 120 and 170 nM). NXPZ-2 dose-dependently attenuates Aβ[1-42]-induced cognitive disturbances, enhances neuronal number and function, and improves pathological alterations in the brain of Alzheimer's disease (AD) mice. NXPZ-2 has potential for studies of Keap1-Nrf2 PPI inhibitors and AD-related disorders.