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JNJ 10181457 dihydrochlorideCat. No. 4019 |
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Chemical Name: 4-[3-[4-[Piperidinyl]but-1-ynyl]benzyl]morpholine dihydrochloride |
Biological Activity
Histamine H3 receptor antagonist (pKi values are 8.15 and 8.93 for rat and human H3 receptors respectively). Increases extracellular norepinephrine and acetylcholine levels in rat frontal cortex but does not stimulate dopamine release. Brain penetrant.Licensing Information
Sold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.Certificate of Analysis / Safety Data Sheet
References
Bonaventure et al (2007) Histamine H3 receptor antagonists: from target identification to drug leads. Biochem.Pharmacol. 73 1084. PMID: 17129577.
Esbenshade et al (2008) The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. Br.J.Pharmacol. 154 1166. PMID: 18469850.
Boggs et al (2009) JNJ-10181457, a selective non-imidazole histamine H3 receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition. Neuropharmacology 56 1131. PMID: 19345233.
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