Discovery of novel neuronal voltage-dependent calcium channel blockers based on emopamil left hand as a bioactive template

Yuichi Suzuki; Noboru Yamamoto; Yoichi Iimura; Koki Kawano; Teiji Kimura; Satoshi Nagato; Koichi Ito; Makoto Komatsu; Yoshihiko Norimine; Manami Kimura; Tetsuyuki Teramoto; Yoshihisa Kaneda; Takeshi Hamano; Tetsuhiro Niidome; Masahiro Yonaga

doi:10.1016/s0960-894x(02)01070-3

Discovery of novel neuronal voltage-dependent calcium channel blockers based on emopamil left hand as a bioactive template

Bioorg Med Chem Lett. 2003 Mar 10;13(5):919-22. doi: 10.1016/s0960-894x(02)01070-3.

Authors

Yuichi Suzuki¹, Noboru Yamamoto, Yoichi Iimura, Koki Kawano, Teiji Kimura, Satoshi Nagato, Koichi Ito, Makoto Komatsu, Yoshihiko Norimine, Manami Kimura, Tetsuyuki Teramoto, Yoshihisa Kaneda, Takeshi Hamano, Tetsuhiro Niidome, Masahiro Yonaga

Affiliation

¹ Tsukuba Research Laboratories, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba-shi, Ibaraki 300-2635, Japan. y5-suzuki@hhc.eisai.co.jp

PMID: 12617921
DOI: 10.1016/s0960-894x(02)01070-3

Abstract

A series of novel neuronal voltage-dependent calcium channel (VDCC) blockers, with inhibitory activity at low micromolar and moderate solubility in water, was discovered by constructing and screening a focused library based on emopamil (1) left hand (ELH) as a bioactive template.

MeSH terms

Animals
Calcium Channel Blockers / chemistry*
Calcium Channel Blockers / pharmacology*
Calcium Channels, N-Type / drug effects*
Combinatorial Chemistry Techniques
Ion Channel Gating / drug effects
Piperazines / chemistry
Rats
Solubility
Stereoisomerism
Structure-Activity Relationship
Synaptosomes / drug effects*
Synaptosomes / metabolism
Verapamil / analogs & derivatives*
Verapamil / chemistry*

Substances

Calcium Channel Blockers
Calcium Channels, N-Type
Piperazines
Verapamil
emopamil