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Vedaclidine (INN, codenamed LY-297,802, NNC 11-1053) is an experimental analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M1 and M4 subtypes, yet an antagonist at the M2, M3 and M5 subtypes. It is orally active and an effective analgesic over 3× the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose. Human trials showed little potential for development of dependence or abuse, and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief.

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  • ベダクリジン (ja)
  • Vedaclidine (en)
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  • ベダクリジン(Vedaclidine)は、ムスカリン性アセチルコリン受容体のアゴニスト及びアンタゴニストとして作用する鎮痛剤である。M1型及びM4型の強力な選択的アゴニスト、M2型、M3型、M5型のアンタゴニストとなる。モルヒネの3倍以上強力な経口鎮痛剤であり、流涎や震え等の副作用は、有効量の何倍も服用した時にしか生じない。ヒトの臨床試験では、依存性はほとんど見られず、神経因性疼痛や癌性疼痛の緩和のための医療現場での利用に向けた研究が続いている。 (ja)
  • Vedaclidine (INN, codenamed LY-297,802, NNC 11-1053) is an experimental analgesic drug which acts as a mixed agonist–antagonist at muscarinic acetylcholine receptors, being a potent and selective agonist for the M1 and M4 subtypes, yet an antagonist at the M2, M3 and M5 subtypes. It is orally active and an effective analgesic over 3× the potency of morphine, with side effects such as salivation and tremor only occurring at many times the effective analgesic dose. Human trials showed little potential for development of dependence or abuse, and research is continuing into possible clinical application in the treatment of neuropathic pain and cancer pain relief. (en)
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