On October 1, 2017, Schwalbe, Tobias; Kaindl, Jonas; Huebner, Harald; Gmeiner, Peter published an article.COA of Formula: C11H14ClNO The title of the article was Potent haloperidol derivatives covalently binding to the dopamine D2 receptor. And the article contained the following:
The dopamine D2 receptor (D2R) is a common drug target for the treatment of a variety of neurol. disorders including schizophrenia. Structure based design of subtype selective D2R antagonists requires high resolution crystal structures of the receptor and pharmacol. tools promoting a better understanding of the protein-ligand interactions. Recently, we reported the development of a chem. activated dopamine derivative (FAUC150) designed to covalently bind the L94C mutant of the dopamine D2 receptor. Using FAUC150 as a template, we elaborated the design and synthesis of irreversible analogs of the potent antipsychotic drug haloperidol forming covalent D2R-ligand complexes. The disulfide- and Michael acceptor-functionalized compounds showed significant receptor affinity and an irreversible binding profile in radioligand depletion experiments The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).COA of Formula: C11H14ClNO
The Article related to preparation haloperidol derivative covalently binding dopamine d2 receptor, chemical probe, covalent ligand, disulfide tethering, dopamine d(2) receptor, g protein-coupled receptor, haloperidol and other aspects.COA of Formula: C11H14ClNO
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem