BTRX-335140 (Navacaprant, CYM-53093) is a potent, selective, orally active κ opioid receptor (KOR) antagonist with IC50 of 0.8 nM.
BTRX-335140 displays >100-fold selectivity over MOR and DOR.
BTRX-335140 demonstrates favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rat pharmacodynamic experiments, shows robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice.
