In 2018,Journal of Medicinal Chemistry included an article by Selvam, Chelliah; Lemasson, Isabelle A.; Brabet, Isabelle; Oueslati, Nadia; Karaman, Berin; Cabaye, Alexandre; Tora, Amelie S.; Commare, Bruno; Courtiol, Tiphanie; Cesarini, Sara; McCort-Tranchepain, Isabelle; Rigault, Delphine; Mony, Laetitia; Bessiron, Thomas; McLean, Heather; Leroux, Frederic R.; Colobert, Francoise; Daniel, Herve; Goupil-Lamy, Anne; Bertrand, Hugues-Olivier; Goudet, Cyril; Pin, Jean-Philippe; Acher, Francine C.. Related Products of 1129-28-8. The article was titled 《Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites》. The information in the text is summarized as follows:
A group III metabotropic glutamate (mGlu) receptor agonist (PCEP) was identified by virtual HTS. This orthosteric ligand is composed by an L-AP4-derived fragment that mimics glutamate and a chain that binds into a neighboring pocket, offering possibilities to improve affinity and selectivity. Herein the authors describe a series of derivatives where the distal chain is replaced by an aromatic or heteroaromatic group. Potent agonists were identified, including some with a mGlu4 subtype preference, e.g., 17m (LSP1-2111) and 16g (LSP4-2022). Mol. modeling suggests that aromatic functional groups may bind at either one of the two chloride regulatory sites. These agonists may thus be considered as particular bitopic/dualsteric ligands. 17m was shown to reduce GABAergic synaptic transmission at striatopallidal synapses. The authors now demonstrate its inhibitory effect at glutamatergic parallel fiber-Purkinje cell synapses in the cerebellar cortex. Although these ligands have physicochem. properties that are markedly different from typical CNS drugs, they hold significant therapeutic potential. In the experimental materials used by the author, we found Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Related Products of 1129-28-8)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Dehydrobromination, Grignard reactions, reductive coupling, Wittig reaction, and several nucleophilic substitution reactions are some of the principal reactions which involve organic bromides. Related Products of 1129-28-8
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary