6-O-(2-[18F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([18F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo

Marjorie R. Levinstein; Emilya N. Ventriglia; Juan L. Gomez; Reece C. Budinich; János Marton; Gjermund Henriksen; Daniel P. Holt; Robert F. Dannals; Martin G. Pomper; Carlos A. Zarate; Jordi Bonaventura; Michael Michaelides

doi:10.1007/s11307-022-01767-5

6-O-(2-[¹⁸F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([¹⁸F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo

Marjorie R. Levinstein, Emilya N. Ventriglia, Juan L. Gomez, Reece C. Budinich, János Marton, Gjermund Henriksen, Daniel P. Holt, Robert F. Dannals, Martin G. Pomper, Carlos A. Zarate, Jordi Bonaventura, Michael Michaelides

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

4 Scopus citations

Abstract

Purpose: 6-O-(2-[¹⁸F]Fluoroethyl)-6-O-desmethyl-diprenorphine ([¹⁸F]FE-DPN) is regarded as a non-selective opioid receptor radiotracer. Procedure: Here, we report the first characterization of [¹⁸F]FE-DPN synthesized from the novel precursor, 6-O-(2-tosyloxyethoxy)-6-O-desmethyl-3-O-trityl-diprenorphine (TE-TDDPN), using a one-pot, two-step nucleophilic radiosynthesis to image opioid receptors in rats and mice using positron emission tomography. Results: We also show that [¹⁸F]FE-DPN and [³H]DPN exhibit negligible brain uptake in mu opioid receptor (MOR) knockout mice. Conclusions: Taken together with prior findings, our results suggest that [¹⁸F]FE-DPN and [³H]DPN preferentially bind to MOR in rodents in vivo.

Original language	English (US)
Pages (from-to)	384-390
Number of pages	7
Journal	Molecular Imaging and Biology
Volume	25
Issue number	2
DOIs	https://doi.org/10.1007/s11307-022-01767-5
State	Published - Apr 2023
Externally published	Yes

Keywords

Diprenorphine
In vivo
Opioid
PET

ASJC Scopus subject areas

Oncology
Radiology Nuclear Medicine and imaging
Cancer Research

Access to Document

10.1007/s11307-022-01767-5

Cite this

Levinstein, M. R., Ventriglia, E. N., Gomez, J. L., Budinich, R. C., Marton, J., Henriksen, G., Holt, D. P., Dannals, R. F., Pomper, M. G., Zarate, C. A., Bonaventura, J., & Michaelides, M. (2023). 6-O-(2-[¹⁸F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([¹⁸F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo. Molecular Imaging and Biology, 25(2), 384-390. https://doi.org/10.1007/s11307-022-01767-5

Levinstein, MR, Ventriglia, EN, Gomez, JL, Budinich, RC, Marton, J, Henriksen, G, Holt, DP, Dannals, RF, Pomper, MG, Zarate, CA, Bonaventura, J & Michaelides, M 2023, '6-O-(2-[¹⁸F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([¹⁸F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo', Molecular Imaging and Biology, vol. 25, no. 2, pp. 384-390. https://doi.org/10.1007/s11307-022-01767-5

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title = "6-O-(2-[18F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([18F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo",

abstract = "Purpose: 6-O-(2-[18F]Fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) is regarded as a non-selective opioid receptor radiotracer. Procedure: Here, we report the first characterization of [18F]FE-DPN synthesized from the novel precursor, 6-O-(2-tosyloxyethoxy)-6-O-desmethyl-3-O-trityl-diprenorphine (TE-TDDPN), using a one-pot, two-step nucleophilic radiosynthesis to image opioid receptors in rats and mice using positron emission tomography. Results: We also show that [18F]FE-DPN and [3H]DPN exhibit negligible brain uptake in mu opioid receptor (MOR) knockout mice. Conclusions: Taken together with prior findings, our results suggest that [18F]FE-DPN and [3H]DPN preferentially bind to MOR in rodents in vivo.",

keywords = "Diprenorphine, In vivo, Opioid, PET",

author = "Levinstein, {Marjorie R.} and Ventriglia, {Emilya N.} and Gomez, {Juan L.} and Budinich, {Reece C.} and J{\'a}nos Marton and Gjermund Henriksen and Holt, {Daniel P.} and Dannals, {Robert F.} and Pomper, {Martin G.} and Zarate, {Carlos A.} and Jordi Bonaventura and Michael Michaelides",

note = "Publisher Copyright: {\textcopyright} 2022, This is a U.S. Government work and not under copyright protection in the US; foreign copyright protection may apply.",

year = "2023",

month = apr,

doi = "10.1007/s11307-022-01767-5",

language = "English (US)",

volume = "25",

pages = "384--390",

journal = "Molecular Imaging and Biology",

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T1 - 6-O-(2-[18F]Fluoroethyl)-6-O-Desmethyl-Diprenorphine ([18F]FE-DPN) Preferentially Binds to Mu Opioid Receptors In Vivo

AU - Levinstein, Marjorie R.

AU - Ventriglia, Emilya N.

AU - Gomez, Juan L.

AU - Budinich, Reece C.

AU - Marton, János

AU - Henriksen, Gjermund

AU - Holt, Daniel P.

AU - Dannals, Robert F.

AU - Pomper, Martin G.

AU - Zarate, Carlos A.

AU - Bonaventura, Jordi

AU - Michaelides, Michael

PY - 2023/4

Y1 - 2023/4

N2 - Purpose: 6-O-(2-[18F]Fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) is regarded as a non-selective opioid receptor radiotracer. Procedure: Here, we report the first characterization of [18F]FE-DPN synthesized from the novel precursor, 6-O-(2-tosyloxyethoxy)-6-O-desmethyl-3-O-trityl-diprenorphine (TE-TDDPN), using a one-pot, two-step nucleophilic radiosynthesis to image opioid receptors in rats and mice using positron emission tomography. Results: We also show that [18F]FE-DPN and [3H]DPN exhibit negligible brain uptake in mu opioid receptor (MOR) knockout mice. Conclusions: Taken together with prior findings, our results suggest that [18F]FE-DPN and [3H]DPN preferentially bind to MOR in rodents in vivo.

AB - Purpose: 6-O-(2-[18F]Fluoroethyl)-6-O-desmethyl-diprenorphine ([18F]FE-DPN) is regarded as a non-selective opioid receptor radiotracer. Procedure: Here, we report the first characterization of [18F]FE-DPN synthesized from the novel precursor, 6-O-(2-tosyloxyethoxy)-6-O-desmethyl-3-O-trityl-diprenorphine (TE-TDDPN), using a one-pot, two-step nucleophilic radiosynthesis to image opioid receptors in rats and mice using positron emission tomography. Results: We also show that [18F]FE-DPN and [3H]DPN exhibit negligible brain uptake in mu opioid receptor (MOR) knockout mice. Conclusions: Taken together with prior findings, our results suggest that [18F]FE-DPN and [3H]DPN preferentially bind to MOR in rodents in vivo.

KW - Diprenorphine

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