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翻訳と辞書　辞書検索 [ 開発暫定版 ] スポンサード リンク AH-1058 ： ウィキペディア英語版 AH-1058 AH-1058 is a lipophilic antiarrhythmic calcium channel blocker synthesized by the Pharmaceutical Research Laboratories of Ajinomoto Co., Inc in Kawasaki, Japan.〔Takahara A, Uneyama H, Noriko U, et al. Effects of AH-1058, A new antiarrhythmic drug, on experimental arrhythmias and cardiac membrane currents. Journal of Cardiovascular Pharmacology 1999; vol 33:625-632〕 It is derived from cyproheptadine, a compound with known antiserotonic, antihistaminic and calcium channel blocking properties.〔〔Hiroshi K, Makoto S, Kazuhide O, et al. On the ionic mechanism of cyproheptadine-induced bradycardia in a rabbit sinoatrial node preparation. European Journal of Pharmacology 1987; vol 139:307-313〕 The IUPAC name of AH-1058 is: 4-(5H-dibenzo()cyclohepten-5-ylidene)-1-(phenyl-2-propenyl )piperidine hydrochloride.〔Takahara A, Sugiyama A, Dohmoto H, et al. Electrophysiological and cardiohemodynamic effects of AH-1058, a new type calicum channel blocker, assessed by the in vivo canine model. Japanese Journal of Pharmacology 2000; vol 83:107-112〕 ==Mechanism of Action== AH-1058 is a cardioselective L-type calcium channel blocker.〔〔〔Tanaka H, Icikawa T, Matsui S, et al. Calcium channel antagonistic effects of AH-1058, a novel antiarrhythmic drug, on guinea-pig myocardium. Res Commun Mol Pathol Pharmacol 1999; vol 104:13-21〕 AH-1058 binds to the same sites on the alpha-1 subunit of L-type calcium channels as phenylalkylamines (ex. verapamil) and benzothiazepines; both of which are well known calcium channel blockers.〔Takahara A, Sugiyama A, Yoshimoto R, et al. AH-1058: A novel cardioselective Ca2+ channel blocker. Cardiovascular Drug Reviews 2001; vol 19:279-296〕 These sites on the alpha-1 subunit differ from the active site of the calcium channel, meaning AH-1058 binds L-type calcium channels allosterically to alter activity.〔 In addition AH-1058 appears to interact with multiple states of L-type calcium channels (i.e. resting and inactive) to suppress calcium currents.〔 A minor effect on sodium channels at higher concentrations has also been seen, but these effects appear to vary between species.〔 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「AH-1058」の詳細全文を読む スポンサード リンク 翻訳と辞書 : 翻訳のためのインターネットリソース Copyright(C) kotoba.ne.jp 1997-2016. All Rights Reserved.