I am a
Home I AM A Search Login

Papers of the Week

Papers: 21 Jan 2023 - 3 Feb 2023

2023 Jan 20

Eur J Pharmacol

Adriforant is a functional antagonist of histamine receptor 4 and attenuates itch and skin inflammation in mice.


Uluckan O, Bruno S, Wang Y, Wack N, Wilzopolski J, Goetschy J-F, Delucis-Bronn C, Urban B, Fehlmann D, Stark H, Hauchard A, Roussel E, Kempf D, Kaupmann K, Raulf F, Bäumer W, Röhn TA, Zerwes H G
Eur J Pharmacol. 2023 Jan 20:175533.
PMID: 36690055.


Histamine has been postulated to play a role in atopic dermatitis via histamine receptor 4, mediating pruritic and inflammatory effects. The H4R antagonist adriforant (PF-3893787 or ZPL389) indicated clinical efficacy in a Ph2a study in atopic dermatitis. Preclinical investigations of adriforant had been scarce as experiments in transfectants with H4R from several species suggested partial agonism, not seen in human cells.