-transparent.png){kind=logo}
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 inhibition by 2d was non-competitive and the inhibition constant (Ki) was 0.80 microM. 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.
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
July 2021,
Bioorganic & medicinal chemistry,
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
October 2015,
Bioorganic & medicinal chemistry,
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
November 2019,
Bioorganic chemistry,
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
February 2010,
Bioorganic & medicinal chemistry,
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
June 2024,
European journal of medicinal chemistry,
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
November 2019,
Molecular diversity,
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
December 2020,
Journal of enzyme inhibition and medicinal chemistry,
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
January 2011,
Bioorganic & medicinal chemistry,
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
June 2020,
Pharmacological reports : PR,
Y Ohmomo, and
K Murakami, and
M Hirata, and
A Sugimoto, and
Y Magata, and
N Miyahara, and
C Tanaka, and
A Yokoyama
July 1984,
The Journal of clinical psychiatry,
