Methopholine

Methopholine

Methopholine is an opioid analgesic drug invented in the 1960s.

Methopholine is an isoquinoline derivative which is not structurally related to most other opioids. It has around the same efficacy as an analgesic as codeine, and was evaluated for the treatment of postoperative pain, but never commercialised. Methopholine has two enantiomers, with the levo (R) enantiomer being the active form, around 3x the potency of codeine, and the (S) enantiomer being inactive. Analogues where the 4'-chloro group has been replaced by other groups have also been tested, the fluoro derivative being slightly more potent than chloro, and the nitro derivative being most potent of all, with the racemic 4'-nitromethopholine being around 20x the potency of codeine.

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