Laboratory of Medicinal Chemistry, IQOG, CSIC , C/Juan de la Cierva 3 , 28006 Madrid , Spain.
Laboratório de Neurologia Experimental , Universidade do Extremo Sul Catarinense , Av. Universitária , 1105 Criciúma , Brazil.
J Med Chem. 2018 Aug 9;61(15):6937-6943. doi: 10.1021/acs.jmedchem.8b00848. Epub 2018 Jul 18.
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 in the radial maze assay in an in vivo Alzheimer's disease test, comparing very favorably with donepezil.
Contilisant 是一种具有通透性、抗氧化和神经保护作用的物质，对 H3R 的亲和力高达纳摩尔水平，对单胺氧化酶和胆碱酯酶具有优异的抑制作用，同时也是一种亲和且选择性的 S1R 激动剂，其亲和力和功能实验结果均证实了这一点，分子建模也验证了这一结果。此外，在体内阿尔茨海默病测试的放射迷宫试验中，Contilisant 可显著恢复 Aβ 诱导的认知缺陷，与多奈哌齐相比具有很大优势。
