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

PAPERS | January 21 - February 3, 2023 | |

Source: Eur J Pharmacol 2023 Jan 20; . doi: 10.1016/j.ejphar.2023.175533Authors: 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

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.

Pubmed ID: http://www.ncbi.nlm.nih.gov/pubmed/36690055?dopt=Abstract