Opioid ligands having delayed long-term antagonist activity: potential pharmacotherapies for opioid abuse.
Buprenorphine is a partial agonist at the micro -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.
Husbands
Stephen M
SM
Department of Pharmacy and Pharmacology, University of Bath, UK. S.M.Husbands@bath.ac.uk
Lewis
John W
JW
D000701:Analgesics, Opioid / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D002047:Buprenorphine / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D004353:Drug Evaluation, Preclinical; D005048:Etorphine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D004091:Hydromorphone / Q000031:analogs & derivatives / Q000494:pharmacology; D008024:Ligands; D009019:Morphinans / Q000737:chemistry / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D017450:Receptors, Opioid, mu / Q000819:agonists / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D019966:Substance-Related Disorders / Q000188:drug therapy*
D000701:Analgesics, Opioid; D008024:Ligands; D009019:Morphinans; D009292:Narcotic Antagonists; D017450:Receptors, Opioid, mu; D002047:Buprenorphine; D005048:Etorphine; D004091:Hydromorphone; C034765:18,19-dihydroetorphine