5910-56-5Relevant articles and documents
Discovery, structure-activity relationship study, and oral analgesic efficacy of cyproheptadine derivatives possessing N-type calcium channel inhibitory activity
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
, p. 5333 - 5339 (2006)
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 lower inhibitory activities against L-type calcium channel, histamine (H1), and serotonin (5-HT2A) receptors than those of Cyp. 13 showed an oral analgesic activity in rat formalin-induced pain model.
NOVEL DIARYLALKENE DERIVATIVES AND NOVEL DIARYLALKANE DERIVATIVES
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Page 16, (2008/06/13)
The invention relates to a compound represented by the following general formula (1) or its analogue, which selectively inhibit N-type calcium channels or its analogue, and to a method for treating pain etc. comprising the compound represented by the following general formula (1) or its analogue to a patient in need of such treatment: wherein, A represents CH=CH, etc., a, b, c and d represents CH etc., R1, R2, R3, R4, R5 and R6 represents H etc., V--W represents C=C, etc., n represents 0 to 3, Y1 represents O etc., B represents--(CH2)vCHR21 wherein v is 0 to 3, R21 represents H, a lower alkyl group or the like, etc., G represents--CO--, a covalent bond, etc., m is 0 to 6, R7 and R8 represents H, a lower alkyl group,--COR18a,--COOR20 wherein R18a and R20 each represents a lower alkyl group or the like, etc.