The histamine H3 receptor as a therapeutic drug target for CNS disorders.
The histamine H3 receptor plays a regulatory role in the pre-synaptic release of histamine and other neurotransmitters, making it an attractive target for CNS indications including cognitive disorders, narcolepsy, ADHD and pain. As more and more H3 antagonists/H3 inverse agonists progress through the clinic, knowledge is gained to define the profile of the 'ideal' compound in terms of specificity, pharmacokinetic parameters and both duration and magnitude of receptor occupancy. Whether a single compound profile for the treatment of different disorders can be defined remains to be seen.
Gemkow
Mark J
MJ
Evotec AG, Schnackenburgallee 114, 22525 Hamburg, Germany. mark.gemkow@evotec.com
Davenport
Adam J
AJ
Harich
Silke
S
Ellenbroek
Bart A
BA
Cesura
Andrea
A
Hallett
David
D
D000818:Animals; D002493:Central Nervous System Diseases / Q000188:drug therapy*; D002986:Clinical Trials as Topic; D016503:Drug Delivery Systems; D055808:Drug Discovery; D054314:Drug Inverse Agonism; D005544:Forecasting; D017442:Histamine Agonists / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D006633:Histamine Antagonists / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D006801:Humans; D008954:Models, Biological; D018100:Receptors, Histamine H3 / Q000187:drug effects* / Q000502:physiology
D017442:Histamine Agonists; D006633:Histamine Antagonists; D018100:Receptors, Histamine H3