Discovery, structure–activity relationship study, and oral analgesic efficacy of cyproheptadine derivatives possessing N-type calcium channel inhibitory activity

T Yamamoto, S Niwa, S Iwayama, H Koganei…

Index: Yamamoto, Takashi; Niwa, Seiji; Iwayama, Satoshi; Koganei, Hajime; Fujita, Shin-ichi; Takeda, Tomoko; Kito, Morikazu; Ono, Yukitsugu; Saitou, Yuki; Takahara, Akira; Iwata, Seinosuke; Yamamoto, Hiroshi; Shoji, Masataka Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 15 p. 5333 - 5339

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Citation Number: 32

Abstract

Antiallergic drug cyproheptadine (Cyp) is known to have inhibitory activities for L-type calcium channels in addition to histamine and serotonin receptors. Since we found that Cyp had an inhibitory activity against N-type calcium channel, Cyp was optimized to obtain more selective N-type calcium channel blocker with analgesic action. As a consequence of the optimization, we found 13 with potent N-type calcium channel inhibitory activity which had ...