Drug intelligence / Profile preview

A-803467

Development stage
Preclinical
Lead developer
Abbott
Modality
Small Molecules
Administration
Intravenous, Intraperitoneal
01

Overview

A-803467 is a **potent and selective small-molecule blocker of the Sodium channel protein type 8 subunit alpha (NaV1.8)**, a tetrodotoxin-resistant voltage-gated sodium channel predominantly expressed in dorsal root ganglion (DRG) neurons. It displays high selectivity, with an IC50 of 8 nM at human NaV1.8 and >100-fold lower activity against other major sodium channel isoforms (NaV1.2, NaV1.3, NaV1.5, NaV1.7). In preclinical models, A-803467 shows significant antinociceptive and antihyperalgesic effects, reducing mechanical allodynia and thermal hyperalgesia in rat models of neuropathic and inflammatory pain. It has no significant effect on acute thermal pain, acute postoperative pain, or motor coordination at effective doses. A-803467 was developed for research purposes, primarily for exploring the role of NaV1.8 in pain signaling and neuronal excitability[1][2][3].

02

Targets

SCN5A (Sodium channel protein type 5 subunit alpha)SCN3A (Sodium channel protein type 3 subunit alpha)SCN2A (Voltage-gated sodium channel protein type 2 subunit alpha)SCN10A (Sodium channel protein type X alpha subunit)SCN9A (Sodium channel protein type 9 subunit alpha)

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