Medicinal Chemical and Pharmacological Aspects of Imidazole-Containing Histamine H3 Receptor Antagonists

The first antagonists known for the histamine H3 receptor were mono-substituted imidazolecontaining compounds like thioperamide. Meanwhile numerous novel leads have been developed possessing improved affinities, selectivities, specificities, and pharmacokinetic properties. Scope and limitations of this promising class are discussed concerning their structure-activity relationships as well as pharmacological and potential therapeutic aspects.