blood-brain

Metformin hydrochloride (1,1-Dimethylbiguanide hydrochloride), a widely used anti-diabetic drug, exhibits potential anti-Y properties by inhibiting the proliferation of various Y cells, including colon and prostate.

Metformin (1,1-Dimethylbiguanide) is an AMPK activator with blood-brain barrier permeability. Metformin may improve glycemic control by increasing insulin sensitivity and decreasing intestinal glucose uptake, and is commonly used in type 2 diabetes research.

Oxybenzone is a UV filter commonly used in tanning and skin protection agents. It is a derivative of benzophenone and is used as an endocrine disrupting chemical that penetrates the placental and blood-brain barriers. It impairs autophagy, alters epigenetic status and disrupts vitamin X-like receptor signaling in apoptotic neuronal cells.

L-DOPA belongs to the category of dopamine precursors, serving as an orally active neurotransmitter metabolic precursor capable of crossing the blood-brain barrier and undergoing conversion to dopamine within the brain. The compound exhibits anti-hyperalgesic properties and finds application in Parkinson's disease research as well as in the induction of disease models.

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.

JNJ-1661010 (Takeda-25) is an effective and specific FAAH inhibitor (IC50: 10/ 12 nM for rat/human), shows >100-fold selectivity for FAAH-1 than FAAH-2.

Physostigmine, a parasympathomimetic alkaloid, is a reversible cholinesterase inhibitor. It extracts from the Calabar bean.

Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.

LM11A-31 dihydrochloride is a water-soluble, non-peptide with high blood-brain barrier permeability.LM11A-31 dihydrochloride, a p75NTR (neurotrophin receptor p75) Ligand, is a potent proNGF (nerve growth factor) antagonist.

Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain. Seltorexant is a high-affinity and selective orexin-2 receptor antagonist (pKi: 8.0 and 8.1 for human and rat OX2R).

DG-041 is an antagonist of high-affinity EP3 receptor (IC50s: 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively). DG-041 inhibits PGE2 facilitation of platelet aggregation and has the blood-brain barrier permeability.

Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.

SB-3CT is a potent and specific gelatinase inhibitor for MMP-2 (Ki = 13.9 nM) and MMP-9 (Ki = 600 nM).

Methylnaltrexone bromide (MOA-728) is one of the newer agents of peripherally-acting μ-opioid antagonists. Methylnaltrexone bromide acts to reverse some of the side effects of opioid drugs such as constipation without affecting analgesia or precipitating withdrawals.

FAUC 213 is a selective full antagonist of the dopamine D4 receptor.

MK-0752, a γ-secretase inhibitor, reduces Aβ40 production(IC50=5 nM).

JNJ-63533054 is a potent and selective agonist of hGPR139 with an EC50 = 16 nM.

Cefoselis Sulfate is a widely used beta-lactam antibiotic.

Carbetocin is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

Carbetocin acetate is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.

MAGL-IN-4 (His121 ARG57) is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) targets the DIX domain of Axin, is an activator of the Wnt/β-catenin signaling pathway and can enhance Axin-LRP6 binding to promote Wnt signaling.

Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.