JNJ-5207852 (JNJ5207852) is a potent, selective antagonist of H3 receptor with pKi of 8.9 and 9.24 for rat and human H3, respectively.
JNJ-5207852 does not bind to human H1, H2 or H4 histamine receptors (pKi <5), as well as 50 GPCRs, ion channels and other drug targets.
JNJ-5207852 increases time spent awake and decreases REM sleep and slow-wave sleep in mice and rats (1-10 mg kg(-1) s.c.), ameliorates PTZ kindling-induced learning and mnemonic deficits in weanling mice.
Physicochemical Properties
M.Wt
316.489
Formula
C20H32N2O
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
1-(4-(3-(piperidin-1-yl)propoxy)benzyl)piperidine
References
1. Apodaca R, et al. J Med Chem. 2003 Aug 28;46(18):3938-44.
2. Barbier AJ, et al. Br J Pharmacol. 2004 Nov;143(5):649-61.
3. Jia F, et al. Neuropharmacology. 2006 Mar;50(4):404-11.
4. Abuhamdah RM, et al. Front Syst Neurosci. 2012 Jul 16;6:54.
