Author:
Ghamari Nakisa,Stark Holger,Hamzeh‐Mivehroud Maryam
Abstract
Abstract
Histamine belongs to the group of biogenic amines and exerts its biological properties mainly mediated by four different G‐protein‐coupled receptor class A subtypes, named H
1
–H
4
receptors. While selective agonists are mainly used for pharmacological experiments, antagonists are widely used in different therapeutic fields. Different generations of H
1
receptor antagonists are mainly used for the treatment of allergic diseases and sleep disturbances, whereas H
2
receptor antagonists became blockbuster drugs in the treatment of stomach ulcers. With the detection of the H
3
receptor, the neurotransmitter properties of histamine have been proven. Despite several approaches, so far only one H
3
receptor antagonist (Pitolisant) got market approval for the orphan disease narcolepsy and for obstructive sleep apnea. The immunomodulatory and anti‐inflammatory properties of H
4
receptor antagonists have raised hopes for new therapeutic approaches in the near future.