Abstract
A principle of opioid pharmacotherapy is that high medication doses should occupy fractionally more opioid receptors that mediate heroin effects. In this preliminary study we examined in vivo μ opioid receptor (μOR) binding in three healthy opioid-dependent volunteers during maintenance on 2 and 16 mg sublingual buprenorphine (BUP) liquid, and after detoxification (0 mg) under double-blind, placebo-controlled conditions, and once in matched controls. Binding measures were obtained with the μOR-selective radioligand [11C]carfentanil (CFN) and PET 4 hrs after BUP administration. BUP induced dose-dependent reductions in μOR availability, 36–50% at 2 mg and 79–95% at 16 mg relative to placebo. Heroin abusers also had greater μOR binding potential in the inferofrontal cortex and anterior cingulate regions during placebo, compared to matched controls. Further studies are warranted to examine the relationship of μOR availability with BUP therapeutic actions, and the clinical implications of increased μOR binding during withdrawal.
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Acknowledgements
This research was supported by USPHS Grant DA000254 from the National Institute on Drug Abuse and a research grant (Joe Young, Sr.) from the State of Michigan. The authors are grateful to Richard Berchou for preparation of liquid buprenorphine doses; Karen Downey for clinical diagnosis; John Hopper for medical oversight; Joy Chudyzinski for data management; Ken Bates for recruiting research volunteers; Ja'Near Mathis for urine toxicology testing; staff of the Neuropsychiatric Research Unit at Wayne State University for clinical data collection; and the technologists at the University of Michigan PET Center for image acquisition and reconstruction.
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Zubieta, JK., Greenwald, M., Lombardi, U. et al. Buprenorphine-Induced Changes in Mu-Opioid Receptor Availability in Male Heroin-Dependent Volunteers: A Preliminary Study. Neuropsychopharmacol 23, 326–334 (2000). https://doi.org/10.1016/S0893-133X(00)00110-X
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DOI: https://doi.org/10.1016/S0893-133X(00)00110-X
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