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.
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Sold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
Histamine H3 receptor antagonists: from target identification to drug leads.
Bonaventure et al.
The histamine H3 receptor: an attractive target for the treatment of cognitive disorders.
Esbenshade et al.
JNJ-10181457, a selective non-imidazole histamine H3 receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition.
Boggs et al.