Daerr, Markus et al. published their research in Medicinal Chemistry Research in 2020 |CAS: 39512-49-7

The Article related to fluorescent gat ligand asymmetry bodipy dye, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 39512-49-7

On April 30, 2020, Daerr, Markus; Allmendinger, Lars; Hoefner, Georg; Wanner, Klaus T. published an article.Synthetic Route of 39512-49-7 The title of the article was Synthesis and biological evaluation of fluorescent GAT-ligands based on asymmetric substituted BODIPY dyes. And the article contained the following:

The present study aimed at the development of fluorescent inhibitors addressing the GABA transporters mGAT1-mGAT4 as potential tool compounds in fluorescence based biol. assays. The design of these fluorescent GAT inhibitors followed the structural motifs common for many GAT1-GAT4 inhibitors publicly known except that the lipophilic domain present in this compounds was replaced by a BODIPY moiety to serve as a fluorescent subunit. The fluorescent compounds obtained that way were tested for their inhibitory potencies and subtype selectivities at the four murine GABA transporter subtypes mGAT1-mGAT4 and for their binding affinity for mGAT1. All BODIPY derivatives displayed only low inhibitory potencies and subtype selectivities at the GABA transport proteins mGAT1-mGAT4, as well as low affinities for mGAT1. Still, compounds were found with reasonable binding affinities towards mGAT1 (pKi ∼ 5.0) and inhibitory potencies at mGAT2 and mGAT4 (pIC50 ∼ 5.0). The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Synthetic Route of 39512-49-7

The Article related to fluorescent gat ligand asymmetry bodipy dye, Pharmacology: Structure-Activity and other aspects.Synthetic Route of 39512-49-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem