Keynote review: histamine H3 receptor antagonists reach out for the clinic.
Antagonists of the histamine H(1) and H(2) receptors have been successful as blockbuster drugs for treating allergic conditions and gastric ulcers, respectively. As such, histamine receptors have made a significant contribution to establishing G-Protein-coupled receptors as the favored drug targets of the industry. In this light, it can easily be understood that the discovery of a third histamine receptor subtype (H(3)R) in 1983 was greeted with considerable excitement. However, characterization of the H(3)R turned out to be far from trivial. In the past five years, molecular biology approaches have given fresh impetus to the H(3)R research field. As a result, H(3)R ligands are where they were anticipated to be 20 years ago: at the center of attention and on the verge of an anticipated breakthrough as the next generation of histaminergic blockbuster drugs. Here, we assess the status of the H(3)R medicinal chemistry programs of the various players in the field, as far as can be deduced from patent applications and scientific literature.
Celanire
Sylvain
S
Department of Chemical Research, Chemin du Foriest, B-1420 Braine-l'Alleud, Belgium.
Wijtmans
Maikel
M
Talaga
Patrice
P
Leurs
Rob
R
de Esch
Iwan J P
IJ
D000818:Animals; D001249:Asthma / Q000188:drug therapy; D001289:Attention Deficit Disorder with Hyperactivity / Q000188:drug therapy; D002493:Central Nervous System Diseases / Q000188:drug therapy; D002986:Clinical Trials as Topic; D003072:Cognition Disorders / Q000188:drug therapy; D004345:Drug Industry; D006633:Histamine Antagonists / Q000627:therapeutic use*; D006801:Humans; D008024:Ligands; D009765:Obesity / Q000188:drug therapy; D018100:Receptors, Histamine H3 / Q000378:metabolism*
D006633:Histamine Antagonists; D008024:Ligands; D018100:Receptors, Histamine H3