Histamine H₃ Receptor Antagonists Go to Clinics

Abstract

Within the recent years novel lead optimisations for histamine H₃ receptor antagonists made their way from bench to bedside. Structure–activity relationships, cross-affinities and side effects as well as pharmacokinetic profiling will be discussed on selected promising compound series. Due to diversity in potential therapeutic applications and in some cases a controversial debate, different indications will be highlighted with the potential and the problems of the test compounds, e.g. sleep-wake disorders, attention-deficient hyperactivity disorder, epilepsy, cognitive impairment, schizophrenia, obesity and neuropathic pain. First data published on clinical trials phase II (IIb) are presented showing proof of concept of H₃ receptor antagonists in narcolepsy and photo-induced epilepsy.