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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.

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.

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.

4-Hydroxyantipyrine is formed during oxidative deamination of aminopyrine.

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.

high affinity agonist of the translocator protein

N-tert-butyl-α-Phenylnitrone ((Z)-N-benzylidene-2-Methylpropan-2-aMine oxide) inhibits COX2 catalytic activity. N-tert-butyl-α-Phenylnitrone((Z)-N-benzylidene-2-Methylpropan-2-aMine oxide) possesses potent reactive oxygen species scavenging, anti-inflammatory, neuroprotective, anti-aging, and anti-diabetic activities, and can penetrate the blood-brain barrier.

Regadenoson (CVT-3146) is an adenosine derivative and selective A2A adenosine receptor agonist with coronary vasodilating activity. Upon administration, regadenoson selectively binds to and activates the A2A adenosine receptor, which induces coronary vasodilation. This leads to an increase in coronary blood flow and enhances myocardial perfusion. Compared to adenosine, regadenoson has a longer half-life and shows higher selectivity towards the A2A adenosine receptor. This agent is a very weak agonist for the A1 adenosine receptor and has negligible affinity for the A2B and A3 adenosine receptors.

MOMIPP is a PIKfyve inhibitor and a macropinocytosis inducer. MOMIPP readily penetrates the blood-brain barrier and is moderately effective in suppressing progression of intracerebral glioblastoma xenografts[1][2].

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

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

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

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.

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.

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.

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.

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.

GNE-0723 is a selective positive allosteric modulator of the NMDA receptor, with an EC50 of 21 nM for GluN2A. It can cross the blood-brain barrier (BBB) and improve outcomes in Dravet syndrome (DS) and Alzheimer's disease (AD).

hMAO-B-IN-4 is a selective, reversible and blood–brain barrier (BBB) penetrable inhibitor of human monoamine oxidase-B (hMAO-B, IC50=0.067 μM, Ki= 0.03 μM, hMAO-A, IC50= 33.82 μM).

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

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

A 1070722 is a potent and selective GSK-3 inhibitor, exhibiting high affinity for both GSK-3α (Ki = 0.6 nM) and GSK-3β (Ki = 0.6 nM). It can penetrate the blood-brain barrier (BBB) and accumulate in brain regions, indicating potential use as a PET radiotracer for quantifying GSK-3 in the brain.