The histamine H3 receptor: from gene cloning to H3 receptor drugs.
Since the cloning of the histamine H(3) receptor cDNA in 1999 by Lovenberg and co-workers, this histamine receptor has gained the interest of many pharmaceutical companies as a potential drug target for the treatment of various important disorders, including obesity, attention-deficit hyperactivity disorder, Alzheimer's disease, schizophrenia, as well as for myocardial ischaemia, migraine and inflammatory diseases. Here, we discuss relevant information on this target protein and describe the development of various H(3) receptor agonists and antagonists, and their effects in preclinical animal models.
Leurs
Rob
R
Division of Medicinal Chemistry, Leiden/Amsterdam Center for Drug Research, Vrije Universiteit Amsterdam, Faculty of Science, de Boelelaan 1083, 1081 HV Amsterdam, The Netherlands. leurs@few.vu.nl
Bakker
Remko A
RA
Timmerman
Henk
H
de Esch
Iwan J P
IJ
D000818:Animals; D003001:Cloning, Molecular / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods; D017442:Histamine Agonists / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D018100:Receptors, Histamine H3 / Q000187:drug effects / Q000235:genetics* / Q000627:therapeutic use*
D017442:Histamine Agonists; D018100:Receptors, Histamine H3