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Mini-Reviews in Medicinal Chemistry
ISSN (Print): 1389-5575
ISSN (Online): 1875-5607
VOLUME: 3
ISSUE: 2
DOI: 10.2174/1389557033405395      Price:  $58









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

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Author(s): Stephen M. Husbands and John W. Lewis
Pages 137-144 (8)
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
Affiliation:
Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK