Solid-phase synthetic strategy and bioevaluation of a labeled δ-opioid receptor ligand Dmt-Tic-Lys for In Vivo imaging

Jatinder S. Josan; David L. Morse; Liping Xu; Maria Trissal; Brenda Baggett; Peg Davis; Josef Vagner; Robert J. Gillies; Victor J. Hruby

doi:10.1021/ol900200k

Solid-phase synthetic strategy and bioevaluation of a labeled δ-opioid receptor ligand Dmt-Tic-Lys for In Vivo imaging

Jatinder S. Josan, David L. Morse, Liping Xu, Maria Trissal, Brenda Baggett, Peg Davis, Josef Vagner, Robert J. Gillies, Victor J. Hruby

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

24 Scopus citations

Abstract

A general solid-phase synthetic strategy is developed to prepare fluorescent and/or lanthanide-labeled derivatives of the δ-opioid receptor (δOR) ligand H-Dmt-Tic-Lys(R)-OH. The high δ-OR affinity {K _i = 3 nM) and desirable in vivo characteristics of the Cy5 derivative 1 suggest its usefulness for structure - function studies and receptor localization and as a high-contrast noninvasive molecular marker for live imaging ex vivo or in vivo.

Original language	English (US)
Pages (from-to)	2479-2482
Number of pages	4
Journal	Organic Letters
Volume	11
Issue number	12
DOIs	https://doi.org/10.1021/ol900200k
State	Published - Jun 18 2009

ASJC Scopus subject areas

Biochemistry
Physical and Theoretical Chemistry
Organic Chemistry

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title = "Solid-phase synthetic strategy and bioevaluation of a labeled δ-opioid receptor ligand Dmt-Tic-Lys for In Vivo imaging",

abstract = "A general solid-phase synthetic strategy is developed to prepare fluorescent and/or lanthanide-labeled derivatives of the δ-opioid receptor (δOR) ligand H-Dmt-Tic-Lys(R)-OH. The high δ-OR affinity {K i = 3 nM) and desirable in vivo characteristics of the Cy5 derivative 1 suggest its usefulness for structure - function studies and receptor localization and as a high-contrast noninvasive molecular marker for live imaging ex vivo or in vivo.",

author = "Josan, {Jatinder S.} and Morse, {David L.} and Liping Xu and Maria Trissal and Brenda Baggett and Peg Davis and Josef Vagner and Gillies, {Robert J.} and Hruby, {Victor J.}",

year = "2009",

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doi = "10.1021/ol900200k",

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AU - Josan, Jatinder S.

AU - Morse, David L.

AU - Xu, Liping

AU - Trissal, Maria

AU - Baggett, Brenda

AU - Davis, Peg

AU - Vagner, Josef

AU - Gillies, Robert J.

AU - Hruby, Victor J.

PY - 2009/6/18

Y1 - 2009/6/18

N2 - A general solid-phase synthetic strategy is developed to prepare fluorescent and/or lanthanide-labeled derivatives of the δ-opioid receptor (δOR) ligand H-Dmt-Tic-Lys(R)-OH. The high δ-OR affinity {K i = 3 nM) and desirable in vivo characteristics of the Cy5 derivative 1 suggest its usefulness for structure - function studies and receptor localization and as a high-contrast noninvasive molecular marker for live imaging ex vivo or in vivo.

AB - A general solid-phase synthetic strategy is developed to prepare fluorescent and/or lanthanide-labeled derivatives of the δ-opioid receptor (δOR) ligand H-Dmt-Tic-Lys(R)-OH. The high δ-OR affinity {K i = 3 nM) and desirable in vivo characteristics of the Cy5 derivative 1 suggest its usefulness for structure - function studies and receptor localization and as a high-contrast noninvasive molecular marker for live imaging ex vivo or in vivo.

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SP - 2479

EP - 2482

JO - Organic Letters

JF - Organic Letters

IS - 12

ER -

Solid-phase synthetic strategy and bioevaluation of a labeled δ-opioid receptor ligand Dmt-Tic-Lys for In Vivo imaging

Abstract

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