selective,blood-brain barrier

Labetalol (Apo-Labetalol) is a mixed alpha beta-adrenergic antagonist.It is used to treat high blood pressure. It can be given by mouth for long term hypertension management or intravenously in severe hypertensive situations. The pharmacokinetics of labetalol is affected by the common CYP2C19 polymorphisms.

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.

Masupirdine free base (SUVN-502 free base) is an orally available 5-HT6 receptor antagonist that crosses the blood-brain barrier, with a Ki value of 2.04 nM for the human 5-HT6 receptor. It is potent and selective, inhibiting multiple targets, and can be used in the study of neurological disorders such as Alzheimer's disease.

Masupirdine mesylate (SUVN-502 mesylate) is a selective 5-HT6 receptor antagonist that crosses the blood-brain barrier and is utilized in the study of neurological disorders such as Alzheimer's disease and dementia.

(1R,2R)-2-PCCA hydrochloride is a potent, selective, and blood-brain-barrier-crossing GPR88 receptor agonist with an EC50 value of 1140 n in striatal membranes of WT mice; it can be used to study the central nervous system.

JHU-083 is an orally available, blood-brain barrier-crossing, selective glutaminase antagonist that improves cognitive performance and normalizes abnormal hippocampal glutaminase activity in APOE4 mice.

Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2 PAM, respectively.Darigabat is used in the study of anxiety disorders and epilepsy.

(R)-PF-04822163 is an isomer of PF-04822163. PF-04822163 is an oral, selective PDE1 inhibitor that can cross the blood-brain barrier. PF-04822163 can be used in studies about nervous system disorders such as attention deficit hyperactivity disorder (ADHD) and Parkinson’s disease.

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.

MPT0G211 is a highly selective and orally active HDAC6 inhibitor (IC50=0.291 nM) that has neuroprotective effects and has shown anti-metastatic activity in human breast cancer cells. MPT0G211 has 1,000 times more affinity for HDAC6 than other HDAC subtypes. MPT0G211 can cross the blood-brain barrier and could be used to improve tau phosphorylation and cognitive deficits in Alzheimer's disease models.

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.

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, and orally active dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier, with Ki values of 10.7 nM for rodent D3R and 11.2 nM for human D3R. It is 80-100 times more selective for D3 receptors than other dopamine receptors, acting on D3 receptors (pKi: 8.0), D2 receptors (pKi: 6.0), 5-HT1B receptors (pKi < 5.2), and 5-HT1D receptors (pKi: 5.9).

DN-1289 is an orally available, blood-brain barrier-crossing, selective and potent inhibitor with an IC50 value of 17 nM for di-leucine zipper kinase (DLK) and 40 nM for leucine zipper-bearing kinase (LZK).DN-1289 significantly inhibited optic nerve crush (ONC)-induced p-c-Jun in a mouse model.

DNL343 is a selective and potent eIF2B activator that crosses the blood-brain barrier and inhibits the assembly of stress granules (SGs) induced by the C9ORF72 dipeptide repeats. DNL343 may be useful in the study of neurodegenerative diseases, such as amyotrophic lateral sclerosis (ALS).

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).

BPN 0026709（MT-228） is a selective, blood-brain barrier-permeable non-muscle myosin II inhibitor. BPN 0026709 demonstrates enhanced tolerability by preferentially targeting NMIIB (KI = 1.5 μM) over CMII (KI = 17 μM), with SmMll MD sharing 83.6% sequence identity with NMllB. BPN 0026709 exhibits sustained efficacy in animal models of stimulant use disorder.

SL327 is a selective inhibitor for MEK1 2 with IC50 of 0.18 μM 0.22 μM; able to transport through the blood-brain barrier.

ASP-2905 is a potent and selective inhibitor of potassium channel Kv12.2 encoded by the Kcnh3 BEC1 gene. It can cross the blood-brain barrier and has antipsychotic activities

SR 57227 hydrochloride(SR 57227A ) is a potent, orally active and selective 5-HT3 receptor agonist. It with ability to cross the blood brain barrier. It has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.

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).

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.

Bozitinib (PLB-1001) (PLB-1001) is a highly selective inhibitor of the c-MET kinase with blood-brain barrier permeability. Bozitinib binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.

CO23 is a blood-brain barrier penetrant and selective TRα agonist and can be used in studies about the regulation of growth and development.

VX-984 (M9831) is an oral, selective DNA-PK inhibitor that can cross the blood-brain barrier. VX-984 inhibited the conjugation of non-homologous terminal NHEJ and acted on DSBs to break DNA double strand. VX-984 is commonly seen in glioblastoma (GBM) and non-small cell lung cancer (NSC-LC) studies.