PF-05198007 / Pfizer - LARVOL DELTA

Examination of the contribution of Nav1.7 to axonal propagation in nociceptors. (PubMed, Pain) - "100-300nM PF-05198007 blocked propagation in 63% of C-fiber sensory neurons, whereas similar concentrations produced minimal block (5%) in rapidly conducting A-fiber neurons. We conclude that Nav1.7 is essential for axonal propagation in around 2/3rds of nociceptive cutaneous C-fiber neurons, and a lower proportion (≤45%) of nociceptive neurons innervating muscle."

Journal • Pain

[VIRTUAL] Examination of the contribution of Nav1.7 to axonal propagation in nociceptors (IASP 2021) - "Nav1.7 was targeted using the selective blocker PF-05198007 (100nM-1µM) and broad spectrum Nav blocker tetrodotoxin (TTX) (50nM-10µM). Our results indicate that Nav1.7 has an essential contribution to axonal propagation in only around 2/3rds of nociceptive C fiber neurons innervating the skin, and a lower proportion (?45%) of nociceptive neurons innervating muscle. Furthermore, we have demonstrated that inflammatory-induced spontaneous activity can occur independently of Nav1.7 and other TTX-S Navs in some neurons. Together, these findings suggest that peripherally restricted Nav1.7 blockers will not be fully effective analgesics for the treatment of certain chronic pain conditions."

Pain