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

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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 ( IF 6.8 ) Pub Date : 2018-07-03 00:00:00 , DOI: 10.1021/acs.jmedchem.8b00848
Óscar M Bautista-Aguilera ₁ , Josiane Budni ₂ , Francielle Mina ₂ , Eduarda Behenck Medeiros ₂ , Winnie Deuther-Conrad ₃ , José M Entrena ₄ , Ignacio Moraleda ₅ , Isabel Iriepa ₅ , Francisco López-Muñoz _{6,

7} , José Marco-Contelles ₁

Affiliation

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_1–42 in the radial maze assay in an in vivo Alzheimer’s disease test, comparing very favorably with donepezil.

中文翻译：

Contilisant，一种用于治疗阿尔茨海默病的四靶点小分子，结合了胆碱酯酶、单胺氧化酶抑制以及 H3R 拮抗作用和 S1R 激动作用

Contilisant 是一种渗透性、抗氧化剂和神经保护剂，对 H3R 表现出高 nM 亲和力，对单胺氧化酶和胆碱酯酶具有出色的抑制作用，根据结合亲和力和功能实验，它是纳摩尔范围内的亲和选择性 S1R 激动剂。通过分子模型证实。此外，在体内阿尔茨海默氏病测试的径向迷宫测定中，Contilisant 显着恢复了由 Aβ _1-42诱导的认知缺陷，与多奈哌齐相比非常有利。

更新日期：2018-07-03

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