alpha-fluoromethylhistidine

Alpha-fluoromethylhistidine (alpha-FMH) is a synthetic small molecule that acts as an irreversible inhibitor of histidine decarboxylase (HDC), the enzyme responsible for converting histidine to histamine. It functions as a "suicide substrate" or Kcat inhibitor by being enzymatically converted to a more active form that irreversibly inactivates HDC. This leads to time-dependent and long-lasting inhibition of histamine synthesis both in vitro and in vivo. Alpha-FMH has been used primarily as a research tool to study the physiological roles of histamine, including its involvement in central nervous system function and pituitary-adrenocortical responses. The compound was initially developed by Merck & Co., Inc., but its clinical development for indications such as pruritus was discontinued after reaching Phase 1 trials[2][4][5][6].

Other names

α-fluoromethylhistidine(S)-alpha-Fluoromethylhistidineα-Fluoromethyl-L-histidine