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JNJ-17216498 is an orally active, investigational small molecule that acts as a selective antagonist of the histamine H3 receptor. It was developed by Johnson & Johnson for the treatment of narcolepsy. The drug targets the histamine H3 receptor (HRH3), which functions as a presynaptic autoreceptor and heteroreceptor in the central nervous system, regulating the release of histamine and other neurotransmitters such as acetylcholine. By antagonizing this receptor, JNJ-17216498 was intended to promote wakefulness and improve symptoms associated with narcolepsy. Clinical development reached Phase 2 trials for narcolepsy but was subsequently discontinued[1][2][3][4][5].
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