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[C-11] Carfentanil Binds Preferentially to mu-Opioid Receptor Subtype 1 Compared to Subtype 2
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
2015 (English)In: Molecular Imaging, ISSN 1535-3508, E-ISSN 1536-0121, Vol. 14, 476-483 p.Article in journal (Refereed) Published
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Abstract [en]

The positron emission tomography (PET) ligand [C-11] carfentanil is a selective agonist for mu-opioid receptors and has been used for studying mu-opioid receptors in the human brain. However, it is unknown if [C-11] carfentanil binding differentiates between subtype receptors mu(1) and mu(2). In this study, we investigated whether mu(1) and mu(2) can be studied separately through receptor subtype-selective inhibition of [C-11] carfentanil by pharmacologic intervention. [C-11] Carfentanil binding characteristics on rat brain sections were assessed either alone or in the presence of the mu-receptor inhibitor cyprodime or the mu(1)-specific inhibitor naloxonazine. [C-11] Carfentanil binding in the living rat brain was similarly studied by small animal PET/computed tomography during baseline conditions or following displacement by cyprodime or naloxonazine. Autoradiography binding studies on rat brain sections demonstrated that [C-11] carfentanil has higher affinity and binding potential for mu(1) than for mu(2). [C-11] Carfentanil binding to mu(2) in vivo could not be detected following specific blocking of mu(1), as predicted from the low binding potential for mu(2) as measured in vitro. [C-11] Carfentanil binding is preferential for mu(1) compared to mu(2) in vitro and in vivo. Clinical studies employing [C-11] carfentanil are therefore likely biased to measure mu(1) rather than mu(2).

Place, publisher, year, edition, pages
2015. Vol. 14, 476-483 p.
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Radiology, Nuclear Medicine and Medical Imaging Medical Biotechnology (with a focus on Cell Biology (including Stem Cell Biology), Molecular Biology, Microbiology, Biochemistry or Biopharmacy)
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URN: urn:nbn:se:uu:diva-271053DOI: 10.2310/7290.2015.00019ISI: 000365597900004PubMedID: 26461068OAI: oai:DiVA.org:uu-271053DiVA: diva2:891084
Available from: 2016-01-05 Created: 2016-01-05 Last updated: 2017-12-01Bibliographically approved

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Eriksson, OlofAntoni, Gunnar

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