Gado, Francesca; Di Cesare Mannelli, Lorenzo; Lucarini, Elena; Bertini, Simone; Cappelli, Elena; Digiacomo, Maria; Stevenson, Lesley A.; Macchia, Marco; Tuccinardi, Tiziano; Ghelardini, Carla; Pertwee, Roger G.; Manera, Clementina published the artcile< Identification of the First Synthetic Allosteric Modulator of the CB2 Receptors and Evidence of Its Efficacy for Neuropathic Pain Relief>, Related Products of 128-09-6, the main research area is oxopyridincycloheptanecarboxamide analgesic allosteric modulator synthesis cannabinoid receptor neuropathic pain.
The direct activation of cannabinoid receptors (CBRs) results in several beneficial effects; therefore several CBRs ligands have been synthesized and tested in vitro and in vivo. However, none of them reached an advanced phase of clin. development due mainly to side effects on the CNS. Medicinal chem. approaches are now engaged to develop allosteric modulators that might offer a novel therapeutic approach to achieve potential therapeutic benefits avoiding inherent side effects of orthosteric ligands. Here we identify the first ever synthesized pos. allosteric modulator (PAM) that targets CB2Rs. The evidence for this was obtained using [3H]CP55940 and [35S]GTPγS binding assays. This finding will be useful for the characterization of allosteric binding site(s) on CB2Rs which will be essential for the further development of CB2R allosteric modulators. Moreover, the new CB2R PAM displayed antinociceptive activity in vivo in an exptl. mouse model of neuropathic pain, raising the possibility that it might be a good candidate for clin. development.
Journal of Medicinal Chemistry published new progress about Analgesics. 128-09-6 belongs to class chlorides-buliding-blocks, and the molecular formula is C4H4ClNO2, Related Products of 128-09-6.
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics