cipralisant

Cipralisant is a small-molecule histamine H3 receptor ligand developed by Gliatech as a highly potent, selective modulator of central histaminergic neurotransmission for cognitive and neuropsychiatric indications, including attention deficit hyperactivity disorder. It was originally characterized as a full H3 receptor antagonist based on its ability to enhance histamine turnover and release in vivo, but subsequent work in recombinant human and rat systems showed it to be a functionally selective ligand with both antagonist and agonist properties at different G protein–coupled signaling pathways. Cipralisant exhibits subnanomolar affinity for the H3 receptor, good oral bioavailability, and low toxicity in preclinical models, but its clinical development was discontinued after early-phase trials without progression to approval.[1][2][5][12][15][16]

Brand names

Perceptin

Other names

cipralisantumcipralisant maleatecipralisant tartrate