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Irdabisant is a selective, orally active small molecule that acts as an inverse agonist and antagonist of the histamine H3 receptor. It was developed for its potential to enhance cognition and promote wakefulness by modulating neurotransmitter release in the brain, particularly dopamine and norepinephrine. Irdabisant has demonstrated high affinity for human (Ki = 2.0 nM) and rat (Ki = 7.2 nM) H3 receptors with over 1000-fold selectivity against other histamine receptor subtypes and a broad panel of other targets. The drug was investigated primarily for cognitive impairment associated with schizophrenia but did not progress beyond early clinical development[1][2][3][4][5][6][7].
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