Reactome | HRH3 binds pitosilant

HRH3 binds pitosilant

Stable Identifier

R-HSA-9692867

Type

Reaction [binding]

Species

Homo sapiens

Compartment

plasma membrane, extracellular region

ReviewStatus

5/5

Locations in the PathwayBrowser

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Signal Transduction (Homo sapiens)

- Signaling by GPCR (Homo sapiens)
  - GPCR ligand binding (Homo sapiens)
    - Class A/1 (Rhodopsin-like receptors) (Homo sapiens)
      - Amine ligand-binding receptors (Homo sapiens)
        
        Histamine receptors (Homo sapiens)
        
        HRH3 binds pitosilant (Homo sapiens)

General

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The histamine H3 receptors (HRH3) mediate the histamine signals in the CNS and peripheral nervous system. It signals through the inhibition of adenylate cyclase and displays high constitutive activity. It functions as an auto- and a hetero-receptor at pre- and post-synaptic membranes and has a profound influence on different neurotransmitter balances (Arrang et al. 1983).

Pitolisant is a selective inverse/agonist/antagonist of HRH3 (Ligneau et al. 2007) and is used to treat type 1 or 2 narcolepsy (Dauvilliers et al. 2013).

Literature References

PubMed ID	Title	Journal	Year
17005916	BF2.649 [1-{3-[3-(4-Chlorophenyl)propoxy]propyl}piperidine, hydrochloride], a nonimidazole inverse agonist/antagonist at the human histamine H3 receptor: Preclinical pharmacology Ligneau, X, Perrin, D, Landais, L, Camelin, JC, Calmels, TP, Berrebi-Bertrand, I, Lecomte, JM, Parmentier, R, Anaclet, C, Lin, JS, Bertaina-Anglade, V, la Rochelle, CD, d'Aniello, F, Rouleau, A, Gbahou, F, Arrang, JM, Ganellin, CR, Stark, H, Schunack, W, Schwartz, JC	J. Pharmacol. Exp. Ther.	2007