1002948-40-4Relevant articles and documents
Synthesis and evaluation of iodinated benzamide derivatives as selective and reversible monoamine oxidase B inhibitors
Ohmomo,Murakami,Hirata,Sugimoto,Magata,Miyahara,Tanaka,Yokoyama
, p. 1789 - 1792 (2007/10/02)
A new series of iodinated analogues of N-(2-aminoethyl)benzamide was synthesized and evaluated for inhibitory potency and specificity toward monoamine oxidase type-B (MAO-B). Among them, N-(2-aminoethyl)-2-chloro-4-iodobenzamide hydrochloride (2d) showed high inhibitory potency and selectivity against MAO-B. The type of MAO-B inhihition by 2d was non-competitive and the inhibition constant (K(i)) was 0.80 μM. Strong and selective in vivo MAO-B inhibition by 2d was also confirmed. The brain MAO-B inhibition by 2d was reversible and the enzyme activity completely returned to the control value 24 h after administration. Compound 2d was, therefore, considered to be a candidate for advanced development as a radioiodinated ligand that may be useful for functional MAO-B studies in the living brain using single photon emission computer tomography.