Kort, Michael E. published the artcileDiscovery and Biological Evaluation of 5-Aryl-2-furfuramides, Potent and Selective Blockers of the Nav1.8 Sodium Channel with Efficacy in Models of Neuropathic and Inflammatory Pain, Application of 4-Amino-2-picoline, the publication is Journal of Medicinal Chemistry (2008), 51(3), 407-416, database is CAplus and MEDLINE.
Nav1.8 (also known as PN3) is a tetrodotoxin-resistant (TTx-r) voltage-gated sodium channel (VGSC) that is highly expressed on small diameter sensory neurons and has been implicated in the pathophysiol. of inflammatory and neuropathic pain. Recent studies using an Nav1.8 antisense oligonucleotide in an animal model of chronic pain indicated that selective blockade of Nav1.8 was analgesic and could provide effective analgesia with a reduction in the adverse events associated with nonselective VGSC blocking therapeutic agents. A series of 5-substituted 2-furfuramides, which are potent, voltage-dependent blockers of the human Nav1.8 channel were prepared and characterized. Selected derivatives, e.g. the N-tolylfurancarboxamide I and the N-(dimethoxyphenyl)furancarboxamide II, also blocked TTx-r sodium currents in rat dorsal root ganglia neurons with comparable potency and displayed >100-fold selectivity vs. human sodium (Nav1.2, Nav1.5, Nav1.7) and human ether-a-go-go (hERG) channels. Following systemic administration, I and II dose-dependently reduced neuropathic and inflammatory pain in exptl. rodent models.
Journal of Medicinal Chemistry published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Application of 4-Amino-2-picoline.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem