Fmoc-His(3-Me)OH derives Histidine-associating compounds with biological activity. Fmoc-His(3-Me)OH, with Fmoc-citrulline-OH, Fmoc-His(1-Me)-OH together, forms tri-peptides and shows vasodilating effect with EC50s of 2.7-4.7 mM in 1.0 mM Phenylephrine (PE)-contracted aorta rings. Fmoc-His(3-Me)OH (resin) also makes Methyl-His-Gly-Lys (His(3-Me)-Gly-Lys), thus acts as an [Ca2+]i inhibitor. Fmoc-His(3-Me)OH methylates NAHIS02, making it unable to block the Alzheimer's Aβ channel.