Navacaprant

Navacaprant (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. Navacaprant distributes well into the CNS and can be used for the research of neuropathy^[1]. IC50 & Target:IC50: 0.8 nM (κOR); 110 nM (μOR); 6500 nM (δOR)^[1] In Vitro:Navacaprant (BTRX-335140) (0-10 μM; 4 h) shows selective antagonist activity towards Kappa Opioid Receptor^[1]. In Vivo:Navacaprant (BTRX-335140) (0.01-3 mg/kg; p.o. once) reduces U69,593- stimulated plasma prolactin secretion to levels of without U69,593 treatment^[1].
Navacaprant (BTRX-335140) (1 mg/kg; i.p. once) blocks U-50488-induced antinociception from hot water^[1].
Pharmacokinetic Parameters of BTRX-335140 in rodents^[1].

	Rats IV 1 mg/kg	Mice IV 3 mg/kg	Rats PO 5 mg/kg	Mice PO 10 mg/kg
CL (mL/min/kg)	105	66.5
t1/2 (h)	1.81	1.91	6.19	2.57
AUC0-t (h?ng/mL)	153	725	265	232
Vss (L/kg)	13.8	7.72
F (%)			30.2	12