Fyfe, Tim J.; Kellam, Barrie; Sykes, David A.; Capuano, Ben; Scammells, Peter J.; Lane, J. Robert; Charlton, Steven J.; Mistry, Shailesh N. published the artcile< Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor>, HPLC of Formula: 2265-92-1, the main research area is structure pharmacokinetics haloperidol dopamine D2 receptor.
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.
Journal of Medicinal Chemistry published new progress about Dopamine D2 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 2265-92-1 belongs to class iodides-buliding-blocks, and the molecular formula is C6H3F2I, HPLC of Formula: 2265-92-1.
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com