Abstract
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
Mini-Reviews in Medicinal Chemistry
Title: Opioid Ligands Having Delayed Long-Term Antagonist Activity: Potential Pharmacotherapies for Opioid Abuse
Volume: 3 Issue: 2
Author(s): Stephen M. Husbands and John W. Lewis
Affiliation:
Keywords: opioid ligands, long-term antagonistic activity, opioid abuse, buprenorphine, methadone
Abstract: 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.
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Cite this article as:
Husbands M. Stephen and Lewis W. John, Opioid Ligands Having Delayed Long-Term Antagonist Activity: Potential Pharmacotherapies for Opioid Abuse, Mini-Reviews in Medicinal Chemistry 2003; 3 (2) . https://dx.doi.org/10.2174/1389557033405395
DOI https://dx.doi.org/10.2174/1389557033405395 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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