structure-activity relationship (SAR)Several series of 伪,伪-disubstituted polycyclic compounds were found to enhance the stimulus-induced release of neurotransmitters, especially acetylcholine, in brain slices. This work resulted in the identification of linopirdine [3,3-bis (4-pyridinylmethyl)-1, 3...
H. (2001). Agonists at the α 4 β 2 nicotinic acetylcholine receptors: Structure-activity relationships and molecular... JE Tønder,PH Olesen - 《Current Medicinal Chemistry》 被引量: 197发表: 2001年 Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl...
GPCR, G protein-coupled receptor; mAChR, muscarinic acetylcholine receptor; SAR, structure–activity relationship. sidtuednytifoief dthoertMho1 srteecreicptaonrd-saellleocsttievreicagfroangimsteTnBtsPoBf also this molecule53. This latter study is of particular relevance bseelceacutisveeTaBgoPnBi,st...
Most of the mutagenic data can be rationalized in the context of this model, and predict testable hypotheses concerning the mechanism by which ligands control the activity of muscarinic receptors. 展开 关键词: Animals Humans Bacteriorhodopsins Receptors, Muscarinic Ligands Epitopes Computer Simulation ...
The structure of migrastatin was determined to be a 14- membered ring macrolide containing a glutarimide, and that work was followed by total synthesis [3ϳ5]. Studies on the structure-activity relationship for cell migration led to the potent derivative, the migrastatin core which consists of ...
In rivastigmine-treated patients, a 37.1% reduction of AChE activity was found in the frontal cortex, while in the parietal cortex reduction was 28.1%. There was a 27.6% reduction in the temporal cortex which, however, was not significant at a statistical threshold corrected for multiple ...
The computational predictions are supported by data obtained from wet experimental tests. The new insights into the binding and structure-activity relationship obtained from this study should be valuable for future rational design of more potent and selective agonists of the alpha7 receptor. 展开 ...
The finding gives a precise mechanistic basis for the developmental waves of activity in the retina.doi:10.1016/j.tins.2005.06.002Richard H Masland... RH Masland - 《Trends in Neurosciences》 被引量: 71发表: 2005年 The relationship between GABA-containing cells and the cholinergic circuitry in ...
The cholinergic system is essential for memory. While degradation of cholinergic pathways characterizes memory-related disorders such as Alzheimer’s disease, the neurophysiological mechanisms linking the cholinergic system to human memory remain unknown
c Structure activity relationship summary of Nemacol analog activity across nematode species and rat VAChT inhibition constants (Ki). C. elegans and Pristionchus pacificus EC50s are derived from biological triplicates (N = 3) with technical duplicate (n = 2) scoring 18 animals per ...