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 Aβ1-42 in the radial maze assay in an in vivo Alzheimer's disease test, comparing very favorably with donepezil.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Bautista-Aguilera ÓM,Budni J,Mina F,Medeiros EB,Deuther-Conrad W,Entrena JM,Moraleda I,Iriepa I,López-Muñoz F,Marco-Contelles Jdoi
10.1021/acs.jmedchem.8b00848subject
Has Abstractpub_date
2018-08-09 00:00:00pages
6937-6943issue
15eissn
0022-2623issn
1520-4804journal_volume
61pub_type
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