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Updated: Aug 9, 2026

Recording Network Activity in Spinal Nociceptive Circuits Using Microelectrode Arrays
Published on: February 9, 2022
Discovery, structure-activity relationship study, and oral analgesic efficacy of cyproheptadine derivatives
Takashi Yamamoto1, Seiji Niwa, Satoshi Iwayama
1Pharmaceutical Research Laboratory, Ajinomoto company Inc., 1-1, Suzuki-cho, Kawasaki-ku, Kawasaki-shi, Japan.
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 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.
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