Pharmacology of α fluoromethylhistidine, a specific inhibitor of histidine decarboxylase

Abstract α-Fluoromethyl-[S]-liistidine (FMH) is a specific and potent inhibitor of histidine decarboxylase, which forms histamine from histidine. It acts selectively and irreversibly by formation of a covalent linkage, possibly with the serine residue in the active site of the enzyme. A single administration of FMH decreases the histamine content only of non-mast cells in the brain and stomach of rodents, but repeated administration gradually decreases the histamine content of mast cells in all tissues. Thus, FMH can be used to deplete histamine in pharmacological studies. As no marked side-effects have been observed during administration of FMH, it may be useful in pathological conditions, such as some allergic diseases, peptic ulcers and mastocytosis, in which excess production of histamine is involved.