BTRX-335140 is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats.
Orally administered BTRX-335140 (CYM-53093) showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice.
|Solubility (25°C)||DMSO ≥ 10 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Tanya L Wallace, et al. Neurobiol Stress. Kappa opioid receptor antagonism protects working memory performance from mild stress exposure in Rhesus macaques
 Elyssa B Margolis, et al. PLoS One. Differential effects of novel kappa opioid receptor antagonists on dopamine neurons using acute brain slice electrophysiology
 Miguel Guerrero, et al. J Med Chem. Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140)
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