| Title : Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile - Bautista-Aguilera_2018_J.Med.Chem_61_6937 |
| Author(s) : Bautista-Aguilera OM , Budni J , Mina F , Medeiros EB , Deuther-Conrad W , Entrena JM , Moraleda I , Iriepa I , Lopez-Munoz F , Marco-Contelles J |
| Ref : Journal of Medicinal Chemistry , 61 :6937 , 2018 |
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Abstract :
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 Abeta1-42 in the radial maze assay in an in vivo Alzheimer's disease test, comparing very favorably with donepezil. |
| PubMedSearch : Bautista-Aguilera_2018_J.Med.Chem_61_6937 |
| PubMedID: 29969030 |
| Inhibitor | Contilisant |
Bautista-Aguilera OM, Budni J, Mina F, Medeiros EB, Deuther-Conrad W, Entrena JM, Moraleda I, Iriepa I, Lopez-Munoz F, Marco-Contelles J (2018)
Contilisant, a Tetratarget Small Molecule for Alzheimer's Disease Therapy Combining Cholinesterase, Monoamine Oxidase Inhibition, and H3R Antagonism with S1R Agonism Profile
Journal of Medicinal Chemistry
61 :6937
Bautista-Aguilera OM, Budni J, Mina F, Medeiros EB, Deuther-Conrad W, Entrena JM, Moraleda I, Iriepa I, Lopez-Munoz F, Marco-Contelles J (2018)
Journal of Medicinal Chemistry
61 :6937