Radiosynthesis of σ Receptor Ligands for Positron Emission Tomography: 11C- and 18F-Labeled Guanidines

Alan A. Wilson; Robert F. Dannals; Hayden T. Ravert; Mark S. Sonders; Eckard Weber; Henry N. Wagner

doi:10.1021/jm00110a017

Radiosynthesis of σ Receptor Ligands for Positron Emission Tomography: ¹¹C- and ¹⁸F-Labeled Guanidines

Alan A. Wilson, Robert F. Dannals, Hayden T. Ravert, Mark S. Sonders, Eckard Weber, Henry N. Wagner

School of Medicine

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

40 Scopus citations

Abstract

A series of analogues of the potent and selective σ receptor ligand 1,3-ditolylguanidine (DTG) were synthesized and demonstrated to have high affinity for the σ receptor as measured by in vitro [³H]DTG displacement studies using guinea pig brain tissue. Three of these 1-aryl-3-(1-adamantyl)guanidines were radiolabeled—two with carbon-11 and one with fluorine-18. Radiochemical yields and specific activities were sufficient for these radiotracers to be used in positron emission tomography imaging of the haloperidol-sensitive σ receptor.

Original language	English (US)
Pages (from-to)	1867-1870
Number of pages	4
Journal	Journal of medicinal chemistry
Volume	34
Issue number	6
DOIs	https://doi.org/10.1021/jm00110a017
State	Published - Jun 1 1991

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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abstract = "A series of analogues of the potent and selective σ receptor ligand 1,3-ditolylguanidine (DTG) were synthesized and demonstrated to have high affinity for the σ receptor as measured by in vitro [3H]DTG displacement studies using guinea pig brain tissue. Three of these 1-aryl-3-(1-adamantyl)guanidines were radiolabeled—two with carbon-11 and one with fluorine-18. Radiochemical yields and specific activities were sufficient for these radiotracers to be used in positron emission tomography imaging of the haloperidol-sensitive σ receptor.",

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AU - Dannals, Robert F.

AU - Ravert, Hayden T.

AU - Sonders, Mark S.

AU - Weber, Eckard

AU - Wagner, Henry N.

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AB - A series of analogues of the potent and selective σ receptor ligand 1,3-ditolylguanidine (DTG) were synthesized and demonstrated to have high affinity for the σ receptor as measured by in vitro [3H]DTG displacement studies using guinea pig brain tissue. Three of these 1-aryl-3-(1-adamantyl)guanidines were radiolabeled—two with carbon-11 and one with fluorine-18. Radiochemical yields and specific activities were sufficient for these radiotracers to be used in positron emission tomography imaging of the haloperidol-sensitive σ receptor.

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Radiosynthesis of σ Receptor Ligands for Positron Emission Tomography: ¹¹C- and ¹⁸F-Labeled Guanidines

Abstract

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