FCH-2996413 (Peripherally restricted HCAD DREADD actuator)

Novel DREADD actuator for the first peripherally restricted DREADD system named the HCAD DREADD system. This system enables precise study of peripheral physiology without CNS interference.

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. To date, relatively few DREADD studies have been conducted in the PNS.

FCH-2996413 has excellent drug-like properties, peripherally restricted pharmacokinetics and clean off-target profiles. The HCAD system has been shown to selectively reduce pain in mice by targeting peripheral tissues of dorsal root ganglion (DRG). Active in vivo. FCH-2996413 is a racemic mixture which includes the racemates AR2599088 ('088) and AR259089 ('089).

rac-(2R,4R)-7-(1H-1,2,3,4-tetrazol-5-yl)-8,9-diazatricyclo[4.3.0.0,2,4]nona-1(6),7-diene