In 2014,Xiao, Jingbo; Free, R. Benjamin; Barnaeva, Elena; Conroy, Jennie L.; Doyle, Trevor; Miller, Brittney; Bryant-Genevier, Marthe; Taylor, Mercedes K.; Hu, Xin; Dulcey, Andres E.; Southall, Noel; Ferrer, Marc; Titus, Steve; Zheng, Wei; Sibley, David R.; Marugan, Juan J. published 《Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists》.Journal of Medicinal Chemistry published the findings.Recommanded Product: Methyl 4-fluoro-3-nitrobenzoate The information in the text is summarized as follows:
The D2 dopamine receptor (D2 DAR) is one of the most validated drug targets for neuropsychiatric and endocrine disorders. However, clin. approved drugs targeting D2 DAR display poor selectivity between the D2 and other receptors, especially the D3 DAR. This lack of selectivity may lead to undesirable side effects. Described are chem. and pharmacol. characterizations of a novel D2 DAR antagonist series with excellent D2 vs. D1, D3, D4, and D5 receptor selectivity. The final probe, 10-Methyl-11-oxo-N-(2-(thiophen-2-yl)ethyl)-10,11-dihydrodibenzo[b,f][1,4]thiazepine-8-carboxamide 5-(S)-oxide, was obtained through a quant. high-throughput screening campaign, followed by medicinal chem. optimization, to yield a selective mol. with good in vitro phys. properties, metabolic stability, and in vivo pharmacokinetics. The optimized mol. may be a useful in vivo probe for studying D2 DAR signal modulation and could also serve as a lead compound for the development of D2 DAR-selective drug-like mols. for the treatment of multiple neuropsychiatric and endocrine disorders. After reading the article, we found that the author used Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9Recommanded Product: Methyl 4-fluoro-3-nitrobenzoate)
Methyl 4-fluoro-3-nitrobenzoate(cas: 329-59-9) belongs to methyl benzoate. Methyl benzoate reacts at both the ring and the ester, depending on the substrate. Electrophiles attack the ring, illustrated by acid-catalysed nitration with nitric acid to give methyl 3-nitrobenzoate.Recommanded Product: Methyl 4-fluoro-3-nitrobenzoateMethyl 4-fluoro-3-nitrobenzoate is used to prepare dimethyl 3-nitro-3′,4-oxydibenzoate by reacting with 3-hydroxy-benzoic acid methyl ester.
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