253306-09-1Relevant academic research and scientific papers
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
Amino acid derivatives and drugs containing the same as the active ingredient
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, (2008/06/13)
The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.
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.
