Discovery of novel brain permeable and G protein-biased beta-1 adrenergic receptor partial agonists for the treatment of neurocognitive disorders was written by Yi, Bitna;Jahangir, Alam;Evans, Andrew K.;Briggs, Denise;Ravina, Kristine;Ernest, Jacqueline;Farimani, Amir B.;Sun, Wenchao;Rajadas, Jayakumar;Green, Michael;Feinberg, Evan N.;Pande, Vijay S.;Shamloo, Mehrdad. And the article was included in PLoS One in 2017.Product Details of 100927-02-4 The following contents are mentioned in the article:
The beta-1 adrenergic receptor (ADRB1) is a promising therapeutic target intrinsically involved in the cognitive deficits and pathol. features associated with Alzheimer’s disease (AD). Evidence indicates that ADRB1 plays an important role in regulating neuroinflammatory processes, and activation of ADRB1 may produce neuroprotective effects in neuroinflammatory diseases. Novel small mol. modulators of ADRB1, engineered to be highly brain permeable and functionally selective for the G protein with partial agonistic activity, could have tremendous value both as pharmacol. tools and potential lead mols. for further preclin. development. The present study describes our ongoing efforts toward the discovery of functionally selective partial agonists of ADRB1 that have potential therapeutic value for AD and neuroinflammatory disorders, which has led to the identification of the mol. STD-101-D1. As a functionally selective agonist of ADRB1, STD-101-D1 produces partial agonistic activity on G protein signaling with an EC50 value in the low nanomolar range, but engages very little beta-arrestin recruitment compared to the unbiased agonist isoproterenol. STD-101-D1 also inhibits the tumor necrosis factor α (TNFα) response induced by lipopolysaccharide (LPS) both in vitro and in vivo, and shows high brain penetration. Other than the therapeutic role, this newly identified, functionally selective, partial agonist of ADRB1 is an invaluable research tool to study mechanisms of G protein-coupled receptor signal transduction. This study involved multiple reactions and reactants, such as 4-(Benzyloxy)-3-methylphenol (cas: 100927-02-4Product Details of 100927-02-4).
4-(Benzyloxy)-3-methylphenol (cas: 100927-02-4) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Product Details of 100927-02-4
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Ether | (C2H5)2O – PubChem