title: Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers.
abstract: The synthesis and structure-activity relationship (SAR) study of a novel series of N-type calcium channel blockers are described. L-Cysteine derivative 2a was found to be a potent and selective N-type calcium channel blocker with IC(50) 0.63 microM on IMR-32 assay. Compound 2a showed analgesic efficacy in the rat formalin-induced pain model by intrathecal and oral administration.
authors.affiliation: Minase Research Institute, Ono Pharmaceutical Co., Ltd., 3-1-1 Sakurai, Shimamoto, Mishima, 618-8585, Osaka, Japan. seko@ono.co.jp
authors.forename: T
authors.initials: T
authors.lastname: Seko
authors.forename: M
authors.initials: M
authors.lastname: Kato
authors.forename: H
authors.initials: H
authors.lastname: Kohno
authors.forename: S
authors.initials: S
authors.lastname: Ono
authors.forename: K
authors.initials: K
authors.lastname: Hashimura
authors.forename: H
authors.initials: H
authors.lastname: Takimizu
authors.forename: K
authors.initials: K
authors.lastname: Nakai
authors.forename: H
authors.initials: H
authors.lastname: Maegawa
authors.forename: N
authors.initials: N
authors.lastname: Katsube
authors.forename: M
authors.initials: M
authors.lastname: Toda
mesh_terms: D000596:Amino Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D020864:Calcium Channels, N-Type / Q000187:drug effects / Q000378:metabolism*; D004195:Disease Models, Animal; D005557:Formaldehyde; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000596:Amino Acids; D000700:Analgesics; D002121:Calcium Channel Blockers; D020864:Calcium Channels, N-Type; D005557:Formaldehyde