N-cyclopropylmethly (CPM) is a common moiety of opioid ligands and often seen with many opioid antagonists, such as naltrexone naltrindole and nalmefene, and some opioid agonists also bear this moiety. It was noticed in our recent studies that many of the CPM-bearing agonists, including full, partial, or mixed agonists, seemed all displaying reduced drug dependence or certain other related side effects, a phenomenon named functional bias of opioid ligands. Based on our structural modeling and analysis, we considered the CPM moiety responsible for both the antagonism and the functionally biased effects of opioid ligands. In this presentation, we will showcase a number of literature examples along with the modeling results to support our hypothesis.

CPM: A potential moiety to reduce opioid dependence

249th National Meeting (2015)

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