JNJ-10181457 (hydrochloride)

JNJ-10181457 is an antagonist of histamine H3 receptors (Kis = 1.17 and 7.08 nM for human and rat receptors, respectively). 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. It also inhibits LPS-induced increases in time spent immobile in the tail suspension test in mice.Formal Name: 4-[[3-[4-(1-piperidinyl)-1-butyn-1-yl]phenyl]methyl]-morpholine, dihydrochloride. CAS Number: 544707-20-2. Synonyms: RWJ 662733. Molecular Formula: C20H28N2O . 2HCl. Formula Weight: 385.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble, Water: soluble. lambdamax: 240, 251 nm. SMILES: N1(CC2=CC=CC(C#CCCN3CCCCC3)=C2)CCOCC1. InChi Code: InChI=1S/C20H28N2O/c1-3-10-21(11-4-1)12-5-2-7-19-8-6-9-20(17-19)18-22-13-15-23-16-14-22/h6,8-9,17H,1,3-5,10-16,18H2. InChi Key: HDRIBIYPLKZUDQ-UHFFFAOYSA-N.