title: Discovery of novel neuronal voltage-dependent calcium channel blockers based on emopamil left hand as a bioactive template.
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.
authors.affiliation: Tsukuba Research Laboratories, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba-shi, Ibaraki 300-2635, Japan. y5-suzuki@hhc.eisai.co.jp
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Suzuki
authors.forename: Noboru
authors.initials: N
authors.lastname: Yamamoto
authors.forename: Yoichi
authors.initials: Y
authors.lastname: Iimura
authors.forename: Koki
authors.initials: K
authors.lastname: Kawano
authors.forename: Teiji
authors.initials: T
authors.lastname: Kimura
authors.forename: Satoshi
authors.initials: S
authors.lastname: Nagato
authors.forename: Koichi
authors.initials: K
authors.lastname: Ito
authors.forename: Makoto
authors.initials: M
authors.lastname: Komatsu
authors.forename: Yoshihiko
authors.initials: Y
authors.lastname: Norimine
authors.forename: Manami
authors.initials: M
authors.lastname: Kimura
authors.forename: Tetsuyuki
authors.initials: T
authors.lastname: Teramoto
authors.forename: Yoshihisa
authors.initials: Y
authors.lastname: Kaneda
authors.forename: Takeshi
authors.initials: T
authors.lastname: Hamano
authors.forename: Tetsuhiro
authors.initials: T
authors.lastname: Niidome
authors.forename: Masahiro
authors.initials: M
authors.lastname: Yonaga
mesh_terms: D000818:Animals; D002121:Calcium Channel Blockers / Q000737:chemistry* / Q000494:pharmacology*; D020864:Calcium Channels, N-Type / Q000187:drug effects*; D020650:Combinatorial Chemistry Techniques; D015640:Ion Channel Gating / Q000187:drug effects; D010879:Piperazines / Q000737:chemistry; D051381:Rats; D012995:Solubility; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013574:Synaptosomes / Q000187:drug effects* / Q000378:metabolism; D014700:Verapamil / Q000031:analogs & derivatives* / Q000737:chemistry*
chemical_list: D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D010879:Piperazines; D014700:Verapamil; C052752:emopamil