219625-66-8Relevant articles and documents
Structure-activity study of L-amino acid-based N-type calcium channel blockers
Seko, Takuya,Kato, Masashi,Kohno, Hiroshi,Ono, Shizuka,Hashimura, Kazuya,Takimizu, Hideyuki,Nakai, Katsuhiko,Maegawa, Hitoshi,Katsube, Nobuo,Toda, Masaaki
, p. 1901 - 1913 (2007/10/03)
Synthesis and structure-activity relationship (SAR) study of L-amino acid-based N-type calcium channel blockers are described. The compounds synthesized were evaluated for inhibitory activity against both N-type and L-type calcium channels focusing on sel
Structure-activity study of L-cysteine-based N-type calcium channel blockers: optimization of N- and C-terminal substituents.
Seko, Takuya,Kato, Masashi,Kohno, Hiroshi,Ono, Shizuka,Hashimura, Kazuya,Takimizu, Hideyuki,Nakai, Katsuhiko,Maegawa, Hitoshi,Katsube, Nobuo,Toda, Masaaki
, p. 915 - 918 (2007/10/03)
Synthesis and structure-activity relationship (SAR) studies of L-cysteine-based N-type calcium channel blockers are described. In the course of exploring SAR of the N- and C-terminal substituents, the L-cysteine derivative was found to be a potent N-type calcium channel blocker with an IC(50) value of 0.14 microM on IMR-32 assay. Compound showed 12-fold selectivity for N-type over L-type calcium channels on AtT-20 assay.