Thompson, Andrew J. published the artcileStructure-Activity Relationships of Quinoxaline-Based 5-HT3A and 5-HT3AB Receptor-Selective Ligands, Name: 2,3,6,7-Tetrachloroquinoxaline, the main research area is quinoxaline preparation serotonin 5HT3 subtype receptor selective ligand.
Until recently, discriminating between homomeric 5-HT3A and heteromeric 5-HT3AB receptors was only possible with ligands that bind in the receptor pore. This study describes the first series of ligands that can discriminate between these receptor types at the level of the orthosteric binding site. During a recent fragment screen, 2-chloro-3-(4-methylpiperazin-1-yl)quinoxaline (VUF10166) was identified as a ligand that displays an 83-fold difference in [3H]granisetron binding affinity between 5-HT3A and 5-HT3AB receptors. Fragment hit exploration, initiated from VUF10166 and 3-(4-methylpiperazin-1-yl)quinoxalin-2-ol, resulted in a series of compounds with higher affinity at either 5-HT3A or 5-HT3AB receptors. These ligands reveal that a single atom is sufficient to change the selectivity profile of a compound At the extremes of the new compounds were 2-amino-3-(4-methylpiperazin-1-yl)quinoxaline (I), which showed 11-fold selectivity for the 5-HT3A receptor, and 2-(4-methylpiperazin-1-yl)quinoxaline, which showed an 8.3-fold selectivity for the 5-HT3AB receptor. These compounds represent novel mol. tools for studying 5-HT3 receptor subtypes and could help elucidate their physiol. roles.
ChemMedChem published new progress about 5-HT3 receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (5-HT3AB). 25983-14-6 belongs to class quinoxaline, name is 2,3,6,7-Tetrachloroquinoxaline, and the molecular formula is C8H2Cl4N2, Name: 2,3,6,7-Tetrachloroquinoxaline.
Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider