Mini-Reviews in Medicinal Chemistry


Opioid Ligands Having Delayed Long-Term Antagonist Activity: Potential Pharmacotherapies for Opioid Abuse

Author(s): Stephen M. Husbands, John W. Lewis.


Buprenorphine is a partial agonist at the μ-opioid receptor with long duration of action and also exhibits delayed antagonist activity. Buprenorphine is finding increasing use as a treatment agent for opioid abuse, though its low efficacy is not well tolerated by all addicts. There is interest in developing a higher efficacy version of buprenorphine and in this mini-review some of the ligands recently discovered, that share with buprenorphine a profile of agonism followed by delayed antagonism, are discussed.

Keywords: opioid ligands, long-term antagonistic activity, opioid abuse, buprenorphine, methadone

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Article Details

Year: 2003
Page: [137 - 144]
Pages: 8
DOI: 10.2174/1389557033405395
Price: $58