10 research outputs found
Contilisant, a Tetratarget Small Molecule for Alzheimer’s Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile
Contilisant, a permeable, antioxidant,
and neuroprotectant agent, showing high nM affinity at H3R and excellent
inhibition of the monoamine oxidases and cholinesterases, is an affine
and selective S1R agonist in the nanomolar range, based on the binding
affinity and functional experiment, a result confirmed by molecular
modeling. In addition, contilisant significantly restores the cognitive
deficit induced by Aβ<sub>1–42</sub> in the radial maze
assay in an in vivo Alzheimer’s disease test, comparing very
favorably with donepezil
Contilisant, a Tetratarget Small Molecule for Alzheimer’s Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile
Contilisant, a permeable, antioxidant,
and neuroprotectant agent, showing high nM affinity at H3R and excellent
inhibition of the monoamine oxidases and cholinesterases, is an affine
and selective S1R agonist in the nanomolar range, based on the binding
affinity and functional experiment, a result confirmed by molecular
modeling. In addition, contilisant significantly restores the cognitive
deficit induced by Aβ<sub>1–42</sub> in the radial maze
assay in an in vivo Alzheimer’s disease test, comparing very
favorably with donepezil