JNJ-10181457

JNJ-10181457 is a selective non-imidazole histamine H3 receptor antagonist developed by Johnson & Johnson. It blocks the histamine H3 receptor (pKi values of 8.93 for human and 8.15 for rat) and increases extracellular levels of norepinephrine and acetylcholine in the rat frontal cortex without significantly affecting dopamine release. The compound is brain-penetrant and has been studied for its effects on cognition and acetylcholine neurotransmission, particularly in preclinical rat models for potential use in treating cognitive deficits and learning disorders where acetylcholine neurotransmission is compromised. It has also shown efficacy in animal models of cognition and improvement of depression-like behaviors, presumably via microglial function regulation. No evidence was found for advanced clinical development or approval in any indication.[1][3][5][7][9]

Other names

JNJ-10181457JNJ10181457JNJ 10181457CAS 544707-19-9CAS544707-19-9CAS-544707-19-9JNJ-10181457 dihydrochlorideJNJ10181457 dihydrochlorideJNJ 10181457 dihydrochloride