Multiple Targeting Approaches on Histamine H3 Receptor Antagonists.

Article Details

Citation

Copy to clipboard

Khanfar MA, Affini A, Lutsenko K, Nikolic K, Butini S, Stark H

Multiple Targeting Approaches on Histamine H3 Receptor Antagonists.

Front Neurosci. 2016 May 30;10:201. doi: 10.3389/fnins.2016.00201. eCollection 2016.

PubMed ID

27303254 [ View in PubMed

]

Abstract

With the very recent market approval of pitolisant (Wakix(R)), the interest in clinical applications of novel multifunctional histamine H3 receptor antagonists has clearly increased. Since histamine H3 receptor antagonists in clinical development have been tested for a variety of different indications, the combination of pharmacological properties in one molecule for improved pharmacological effects and reduced unwanted side-effects is rationally based on the increasing knowledge on the complex neurotransmitter regulations. The polypharmacological approaches on histamine H3 receptor antagonists on different G-protein coupled receptors, transporters, enzymes as well as on NO-signaling mechanism are described, supported with some lead structures.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Pitolisant	Histamine H3 receptor	Protein	Humans	Yes	Antagonist Inverse agonist	Details