Journal
BIOLOGICAL & PHARMACEUTICAL BULLETIN
Volume 31, Issue 12, Pages 2163-2181Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.31.2163
Keywords
histamine H-3; sleep disorder; cognition; schizophrenia; obesity; tiprolisant
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Within the recent years novel lead optimisations for histamine H-3 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 H-3 receptor antagonists in narcolepsy and photoinduced epilepsy.
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