Designing Functionally Selective Noncatechol Dopamine D1 Receptor Agonists with Potent In Vivo Antiparkinsonian Activity was written by Martini, Michael L.;Ray, Caroline;Yu, Xufen;Liu, Jing;Pogorelov, Vladimir M.;Wetsel, William C.;Huang, Xi-Ping;McCorvy, John D.;Caron, Marc G.;Jin, Jian. And the article was included in ACS Chemical Neuroscience in 2019.Reference of 175205-82-0 This article mentions the following:
Dopamine receptors are important G protein-coupled receptors (GPCRs) with therapeutic opportunities for treating Parkinson’s Disease (PD) motor and cognitive deficits. Biased D1 dopamine ligands that differentially activate G protein over 闁?arrestin recruitment pathways are valuable chem. tools for dissecting pos. vs. neg. effects in drugs for PD. Here, we reveal an iterative approach toward modification of a D1-selective noncatechol scaffold critical for G protein-biased agonism. This approach provided enhanced understanding of the structural components critical for activity and signaling bias and led to the discovery of several novel compounds with useful pharmacol. properties, including three highly GS-biased partial agonists. Administration of a potent, balanced, and brain-penetrant lead compound from this series results in robust antiparkinsonian effects in a rodent model of PD. This study suggests that the noncatechol ligands developed through this approach are valuable tools for probing D1 receptor signaling biol. and biased agonism in models of neurol. disease. In the experiment, the researchers used many compounds, for example, 2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0Reference of 175205-82-0).
2-Bromo-3-(trifluoromethyl)pyridine (cas: 175205-82-0) belongs to pyridine derivatives. Pyridines are an important class of heterocycles and occur in polysubstituted forms in many naturally occurring biologically active compounds, drug molecules and chiral ligands. Pyridine groups exist in countless molecules, and their applications include catalysis, drug design, molecular recognition, and natural product synthesis.Reference of 175205-82-0