PF 04531083

Description: PF 04531083 is a novel, potent and selective NaV1.8 blocker used for the research of neuropathic/inflammatory pain. Voltage-gated sodium channels (Navs) are an important family of transmembrane ion channel proteins and Nav drug discovery is an exciting field. Pharmaceutical investment in Navs for pain therapeutics has expanded exponentially due to genetic data such as SCN10A mutations and an improved ability to establish an effective screen sequence for example IonWorks Barracuda, Synchropatch and Qube. Moreover, emerging clinical data (AZD-3161, XEN402, CNV1014802, PF-05089771, PF-04531083) combined with recent breakthroughs in Nav structural biology pave the way for a future of fruitful prospective Nav drug discovery.

References: Bioorg Med Chem Lett. 2014 Aug 15; 24(16):3690-9.