bbb penetration

LY 344864, a specifc receptor agonist, is an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.

BuChE-IN-TM-10 (TM-10) is a potent inhibitor of butyrylcholinesterase (BuChE) with an IC50 of 8.9 nM. It effectively inhibits and disaggregates self-induced Aβ aggregation, exhibits significant antioxidant activity, and demonstrates substantial penetration through the blood-brain barrier (BBB), holding promise as a potential treatment for Alzheimer's disease.

Nav1.1 activator 1 is a highly potent activator of Nav1.1 with BBB penetration.

Flucopride (Compound 4a) acts as an acetylcholinesterase inhibitor (AChE) with an IC50 value of 24 nM and serves as a partial agonist for the human 5-HT4 receptor (5-HT4R) with a Ki of 9.6 nM for (h)5-HT4R. It promotes non-amyloidogenic processing of APP in COS-7 cells transiently expressing (h)5-HT4R with an EC50 of 23.0 nM. Flucopride is also likely to exhibit significant gastrointestinal tract (GIT) penetration and blood-brain barrier (BBB) permeability, as determined in PAMPA experiments.

NRMA-9 is an amide prodrug of small molecule nuclear receptor modulators. It shows high exposure levels in the brain, indicating good penetration of the blood-brain barrier (BBB). NRMA-9 is utilized in research related to central nervous system diseases associated with nuclear receptors, such as Alzheimer's and Parkinson's.

NRMA-I is an amide prodrug of a small molecule nuclear receptor modulator. It demonstrates high brain exposure, indicating effective blood-brain barrier (BBB) penetration. NRMA-I is useful for research into central nervous system diseases related to nuclear receptors, such as Alzheimer's and Parkinson's diseases.

GSK-3β inhibitor 9 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC 50 of 35 nM. GSK-3β inhibitor 9 exhibits good pharmacokinetic profiles including favorable BBB penetration. GSK-3β inhibitor 9 is able to be used for the research of Alzheimer's disease [1].

Compound 16 (hAChE Aβ1-42-IN-1) is a potent inhibitor targeting both hAChE and Aβ1-42 aggregation, demonstrating considerable safety in hepG2 cell lines and excellent brain-blood barrier (BBB) penetration with a broad safety margin. This compound shows promise for Alzheimer's disease (AD) research [1].

BuChE-IN-2 is an excellent inhibitor of butylcholinesterase (BuChE) with IC50 values of 1.28 μM for BuChE and 0.67 μM for NO. It inhibits Aβ aggregation, ROS formation, and Cu2+ chelation, shows proper blood-brain barrier (BBB) penetration, and is suitable for Alzheimer's disease research.