JNJ-10181457 (hydrochloride)

JNJ-10181457 is an antagonist of histamine H₃ receptors (K_is = 1.17 and 7.08 nM for human and rat receptors, respectively).¹ It increases extracellular norepinephrine and acetylcholine levels in the frontal cortex of rats when administered subcutaneously at a dose of 10 mg/kg. JNJ-10181457 (1.25-10 mg/kg, p.o.) reduces the number of cataplectic attacks and time spent in cataplexy in familial narcoleptic Dobermans. In mice, JNJ-10181457 (10 mg/kg) decreases the time spent in the open areas of the elevated zero maze, as well as increases locomotor activity in an open field test.² It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.³

WARNING This product is not for human or veterinary use.

1. Bonaventure, P., Letavic, M., Dugovic, C., et al. Histamine H3 receptor antagonists: From target identification to drug leads. Biochem. Pharmacol. 73(8), 1084-1096 (2007).

2. Mohsen, A., Yoshikawa, T., Miura, Y., et al. Mechanism of the histamine H3 receptor-mediated increase in exploratory locomotor activity and anxiety-like behaviours in mice. Neuropharmacology 81, 188-194 (2014).

3. Iida, T., Yoshikawa, T., Kárpáti, A., et al. JNJ10181457, a histamine H3 receptor inverse agonist, regulates in vivo microglial functions and improves depression-like behaviours in mice. Biochem. Biophys. Res. Commun. 488(3), 534-540 (2017).