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Mirfentanil : ウィキペディア英語版
Mirfentanil

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Mirfentanil is a fentanyl derivative with strong selectivity for the μ opioid receptor. At lower doses, it antagonizes the analgesic effects of alfentanil and substitutes for naloxone in morphine-treated monkeys; however, it also reverses naloxone-precipitated withdrawal in pigeons trained to discriminate morphine from naloxone.〔France CP, Winger G, Medzihradsky F, Seggel MR, Rice KC, Woods JH. "Mirfentanil: pharmacological profile of a novel fentanyl derivative with opioid and nonopioid effects." ''Journal of Pharmacology and Experimental Therapeutics''. 1991 Aug;258(2):502-10. PMID 1650830〕
At high doses, it exhibits analgesic activity which is not fully reversed by opioid antagonists, suggesting that the drug has both opioid and non-opioid mechanisms of action.〔〔Carr DJ, Brockunier LL, Scott M, Bagley JR, France CP. "Mirfentanil antagonizes morphine-induced suppression of splenic NK activity in mice." ''Immunopharmacology''. 1996 Aug;34(1):9-16. PMID 8880221〕
Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.
== Synthesis ==
Mirfentanil was synthesized via acylation of the product of the reaction of 2-chloropyrazine and 1-(2-phenylethyl)-4-piperidinone oxime with 2-Furoyl chloride.

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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