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Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.

Spermine (N3BBB), a click chemistry reagent with an azide group, facilitates diverse biochemical studies [1].

Debio 0932 (CUDC-305) is a heat shock protein 90 (Hsp90) inhibitor that targets the n-terminal atp-binding pocket to promote apoptosis, and has the advantage of being orally available and able to cross the blood-brain barrier (BBB) for the treatment of cancers such as non-small-cell lung cancer (NSCLC) and neuroblastoma.

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.

pCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride) is an inhibitor of tryptophan hydroxylase inhibitor and 5-HT synthesis. pCPA methyl ester hydrochloride is permeable across the blood-brain barrier and reduces 5-HT central availability.

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.

Rivastigmine (Exelon) is a Cholinesterase Inhibitor, used for therapy of Alzheimer disease.

Pramipexole dihydrochloride hydrate (Mirapex) is the hydrochloride salt of pramipexole, a benzothiazole derivative. As a nonergot dopamine agonist, pramipexole binds to D2 and D3 dopamine receptors in the striatum and substantia nigra of the brain.

Rivastigmine tartrate (SDZ-ENA 713) is a carbamate-derived reversible CHOLINESTERASE INHIBITOR that is selective for the CENTRAL NERVOUS SYSTEM and is used for the treatment of DEMENTIA in ALZHEIMER DISEASE and PARKINSON DISEASE.

4-Hydroxyantipyrine is formed during oxidative deamination of aminopyrine.

J-147 is an experimental drug with reported effects against both Alzheimer's disease and ageing in mouse models of accelerated aging. It is a curcumin derivative and a potent neurogenic and neuroprotective drug candidate initially developed for the treatment of neurodegenerative conditions associated with aging that impacts many pathways implicated in the pathogenesis of diabetic neuropathy.

Nitrobenzylthioinosine (NBMPR) is an inhibitor of ENT1 transporter that binds to ENT1 transporter with high affinity.

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

Perhexiline is an orally active inhibitor of CPT1 and CPT2 that reduces fatty acid metabolism. Perhexiline can cross the blood-brain barrier (BBB) and exhibits anti-tumor activity. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatocytes. Therefore, Perhexiline can be used in cancer and cardiovascular disease research [1] [2] [5].

AS057278 (3-Methylpyrazole-5-carboxylic acid) is an D-amino acid oxidase (DAAO) inhibitor.

P7C3-A20, a derivative of P7C3, exhibits both proneurogenic and neuroprotective activities (brackets).

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

LY2886721, a BACE inhibitor, is used for the therapy of Alzheimer's Disease.

Irdabisant (CEP-26401) (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant antagonist inverse agonist of histamine H3 receptor (H3R) (rat H3R Ki= 7.2 nM, human H3R Ki= 2.0 nM). Irdabisant exhibits relatively low inhibitory activity against hERG current (IC50= 13.8 μM). Irdabisant exhibits cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used for research on schizophrenia or cognitive impairment.

Baclofen hydrochloride (4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride) is a GAMMA-AMINOBUTYRIC ACID derivative that is a specific GABA-B RECEPTORS agonist. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

Rabies Virus Glycoprotein (TFA), a 29-amino acid-derived cell-penetrating peptide from the Rabies Virus Glycoprotein, can cross the blood-brain barrier (BBB) and enter brain cells.

MS48107 is a potent, selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68), demonstrating specificity for GPR68 over closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. It effectively crosses the blood-brain barrier (BBB) in mice.

high affinity agonist of the translocator protein