Dhanya, Raveendra-Panickar; Sheffler, Douglas J.; Dahl, Russell; Davis, Melinda; Lee, Pooi San; Yang, Li; Nickols, Hilary Highfield; Cho, Hyekyung P.; Smith, Layton H.; D’Souza, Manoranjan S.; Conn, P. Jeffrey; Der-Avakian, Andre; Markou, Athina; Cosford, Nicholas D. P. published the artcile< Design and Synthesis of Systemically Active Metabotropic Glutamate Subtype-2 and -3 (mGlu2/3) Receptor Positive Allosteric Modulators (PAMs): Pharmacological Characterization and Assessment in a Rat Model of Cocaine Dependence>, Reference of 3964-57-6, the main research area is phenoxybutoxy benzoic acid preparation metabotropic glutamate receptor allosteric modulator.
As part of our ongoing small-mol. metabotropic glutamate (mGlu) receptor pos. allosteric modulator (PAM) research, we performed structure-activity relationship (SAR) studies around a series of group II mGlu PAMs. Initial analogs exhibited weak activity as mGlu2 receptor PAMs and no activity at mGlu3. Compound optimization led to the identification of potent mGlu2/3 selective PAMs with no in vitro activity at mGlu1,4-8 or 45 other CNS receptors. In vitro pharmacol. characterization of representative compound I indicated agonist-PAM activity toward mGlu2 and PAM activity at mGlu3. The most potent mGlu2/3 PAMs were characterized in assays predictive of ADME/T and pharmacokinetic (PK) properties, allowing the discovery of systemically active mGlu2/3 PAMs. On the basis of its overall profile, compound II was selected for behavioral studies and was shown to dose-dependently decrease cocaine self-administration in rats after i.p. administration. These mGlu2/3 receptor PAMs have significant potential as small mol. tools for investigating group II mGlu pharmacol.
Journal of Medicinal Chemistry published new progress about Drug dependence. 3964-57-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, Reference of 3964-57-6.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics