Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO

János Marton; Bent W. Schoultz; Trine Hjoernevik; Alexander Drzezga; Behrooz H. Yousefi; Hans Jurgen Wester; Frode Willoch; Gjermund Henriksen

doi:10.1021/jm900892x

Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [¹¹C]PEO

János Marton, Bent W. Schoultz, Trine Hjoernevik, Alexander Drzezga, Behrooz H. Yousefi, Hans Jurgen Wester, Frode Willoch, Gjermund Henriksen

Chair of Pharmaceutical Radiochemistry

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

Abstract

Antagonist radiotracers have shown only a low sensitivity for detecting competition from high-efficacy agonists at opioid receptors (ORs) in vivo. We report that [¹¹C]PEO binds with high affinity to μ and κ-opioid receptors, is a full agonist, and concentrates in brain regions of rats with a high density of the μ-OR after intravenous injection. Blocking studies with μ and κ-OR selective compounds demonstrated that the binding of [¹¹C]PEO is saturable and selective to the μ-OR in rat brain.

Original language	English
Pages (from-to)	5586-5589
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	52
Issue number	18
DOIs	https://doi.org/10.1021/jm900892x
State	Published - 24 Sep 2009

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10.1021/jm900892x

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title = "Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [11C]PEO",

abstract = "Antagonist radiotracers have shown only a low sensitivity for detecting competition from high-efficacy agonists at opioid receptors (ORs) in vivo. We report that [11C]PEO binds with high affinity to μ and κ-opioid receptors, is a full agonist, and concentrates in brain regions of rats with a high density of the μ-OR after intravenous injection. Blocking studies with μ and κ-OR selective compounds demonstrated that the binding of [11C]PEO is saturable and selective to the μ-OR in rat brain.",

author = "J{\'a}nos Marton and Schoultz, \{Bent W.\} and Trine Hjoernevik and Alexander Drzezga and Yousefi, \{Behrooz H.\} and Wester, \{Hans Jurgen\} and Frode Willoch and Gjermund Henriksen",

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T1 - Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors

T2 - [11C]PEO

AU - Marton, János

AU - Schoultz, Bent W.

AU - Hjoernevik, Trine

AU - Drzezga, Alexander

AU - Yousefi, Behrooz H.

AU - Wester, Hans Jurgen

AU - Willoch, Frode

AU - Henriksen, Gjermund

PY - 2009/9/24

Y1 - 2009/9/24

N2 - Antagonist radiotracers have shown only a low sensitivity for detecting competition from high-efficacy agonists at opioid receptors (ORs) in vivo. We report that [11C]PEO binds with high affinity to μ and κ-opioid receptors, is a full agonist, and concentrates in brain regions of rats with a high density of the μ-OR after intravenous injection. Blocking studies with μ and κ-OR selective compounds demonstrated that the binding of [11C]PEO is saturable and selective to the μ-OR in rat brain.

AB - Antagonist radiotracers have shown only a low sensitivity for detecting competition from high-efficacy agonists at opioid receptors (ORs) in vivo. We report that [11C]PEO binds with high affinity to μ and κ-opioid receptors, is a full agonist, and concentrates in brain regions of rats with a high density of the μ-OR after intravenous injection. Blocking studies with μ and κ-OR selective compounds demonstrated that the binding of [11C]PEO is saturable and selective to the μ-OR in rat brain.

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U2 - 10.1021/jm900892x

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SN - 0022-2623

VL - 52

SP - 5586

EP - 5589

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 18

ER -

Synthesis and evaluation of a full-agonist orvinol for PET-imaging of opioid receptors: [¹¹C]PEO

Abstract

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