FCH-2996413 (Peripherally restricted HCAD DREADD actuator)

Novel DREADD actuator for the first peripherally restricted DREADD system (HCAD DREADD). Unlike other DREADD ligands (e.g. CNO & DCZ), FCH-2996413 does not cross the BBB so is able to selectively activate the peripherally restricted HCAD G_i-DREADD. This system enables precise study of peripheral physiology without CNS interference. FCH-2996413 has excellent drug-like properties, peripherally restricted pharmacokinetics and clean off-target profiles. Shown to selectively reduce pain in mice by targeting peripheral tissues of dorsal root ganglion (DRG). Active in vivo. Racemic mixture.