925137-17-3Relevant academic research and scientific papers
11-OXO-10,11-DIHYDRODIBENZO[B,F][1,4]THIAZEPINE S-OXIDE DERIVATIVES AND THEIR USE AS DOPAMINE D2 RECEPTOR ANTAGONISTS
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Paragraph 0235, (2015/02/25)
The disclosure includes compounds and pharmaceutically acceptable salts of Formula (I). Certain compounds and salts of Formula (I) are selective inhibitors of the Dopamine D2 receptor. The variables R1-R4, n, and L are defined herein. The disclosure also provides methods of synthesizing compounds of Formula (I) and pharmaceutical compositions containing compounds of Formula (I). Additionally the disclosure provides methods or treating patients suffering from central nervous system disorders, including Tourette's syndrome, bipolar disorder, hyperprolactinemia, tardive dyskinesia, Huntington's chorea, psychosis, depression, or schizophrenia.
Discovery, optimization, and characterization of novel D2 dopamine receptor selective antagonists
Xiao, Jingbo,Free, R. Benjamin,Barnaeva, Elena,Conroy, Jennie L.,Doyle, Trevor,Miller, Brittney,Bryant-Genevier, Marthe,Taylor, Mercedes K.,Hu, Xin,Dulcey, Andrés E.,Southall, Noel,Ferrer, Marc,Titus, Steve,Zheng, Wei,Sibley, David R.,Marugan, Juan J.
, p. 3450 - 3463 (2014/05/20)
The D2 dopamine receptor (D2 DAR) is one of the most validated drug targets for neuropsychiatric and endocrine disorders. However, clinically approved drugs targeting D2 DAR display poor selectivity between the D2 and other receptors, especially the D3 DA
