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JNJ 10181457 dihydrochloride

Names

[ CAS No. ]:
544707-20-2

[ Name ]:
JNJ 10181457 dihydrochloride

[Synonym ]:
4-{3-[4-(1-Piperidinyl)-1-butyn-1-yl]benzyl}morpholine dihydrochloride
Morpholine, 4-[[3-[4-(1-piperidinyl)-1-butyn-1-yl]phenyl]methyl]-, hydrochloride (1:2)

Biological Activity

[Description]:

JNJ 10181457 is a neutral, potent and selective, brain penetrant H3 antagonist with pKi of 8.93, pA2 of 9.22 for hH3; promotes wakefulnessm, but does not increase locomotor activity or produce any alteration of the EEG power spectral activity in rats; increases extracellular acetylcholine and norepinephrine but not dopamine in rat frontal cortex and shows efficacy in various models of learning-memory deficit.

[References]

References 1. Bonaventure P, et al. Biochem Pharmacol. 2007 Apr 15;73(8):1084-96. 2. Galici R, et al. Neuropharmacology. 2009 Jun;56(8):1131-7. 3. Vanhanen J, et al. Br J Pharmacol. 2013 Sep;170(1):177-87. View Related Products by Target Histamine Receptor

Chemical & Physical Properties

[ Molecular Formula ]:
C20H28N2O.2HCl

[ Molecular Weight ]:
385.371

[ Exact Mass ]:
384.173523


Related Compounds