Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor was written by Fyfe, Tim J.;Kellam, Barrie;Sykes, David A.;Capuano, Ben;Scammells, Peter J.;Lane, J. Robert;Charlton, Steven J.;Mistry, Shailesh N.. And the article was included in Journal of Medicinal Chemistry in 2019.Application In Synthesis of 1,2-Difluoro-3-iodobenzene This article mentions the following:
Haloperidol is a typical antipsychotic drug (APD) associated with an increased risk of extrapyramidal side-effects (EPS) and hyperprolactinemia relative to atypical APDs such as clozapine. Both drugs are dopamine D2 receptor (D2R) antagonists, with contrasting kinetic profiles. Haloperidol displays fast association/slow dissociation at the D2R whereas clozapine exhibits relatively slow association/fast dissociation Recently, the authors have provided evidence that slow dissociation from the D2R predicts hyperprolactinemia, whereas fast association predicts EPS. Unfortunately, clozapine can cause severe side-effects independent of its D2R action. The results suggest an optimal kinetic profile for D2R antagonist APDs that avoids EPS. To begin exploring this hypothesis, the authors conducted a structure-kinetic relationship study of haloperidol and reveal that subtle structural modifications dramatically change binding kinetic rate constants, affording compounds with a clozapine-like kinetic profile. Thus, optimization of these kinetic parameters may allow development of novel APDs based on the haloperidol scaffold with improved side-effect profiles. In the experiment, the researchers used many compounds, for example, 1,2-Difluoro-3-iodobenzene (cas: 64248-57-3Application In Synthesis of 1,2-Difluoro-3-iodobenzene).
1,2-Difluoro-3-iodobenzene (cas: 64248-57-3) belongs to iodide derivatives. Iodide-containing intermediates are common in organic synthesis, because of the easy formation and cleavage of the C–I bond. Polyiodoorganic compounds are sometimes employed as X-ray contrast agents, in fluoroscopy, a type of medical imaging. This application exploits the X-ray absorbing ability of the heavy iodine nucleus.Application In Synthesis of 1,2-Difluoro-3-iodobenzene
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com