Preparation of [11C]- and [125I]IMB: a dopamine D-2 receptor antagonist

Alan A. Wilson; Robert F. Dannals; Hayden T. Ravert; Henry N. Wagner

doi:10.1016/0883-2889(89)90199-8

Preparation of [¹¹C]- and [¹²⁵I]IMB: a dopamine D-2 receptor antagonist

Alan A. Wilson, Robert F. Dannals, Hayden T. Ravert, Henry N. Wagner

School of Medicine

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

6 Scopus citations

Abstract

A new dopamine D-2 receptor ligand, N-[2-(N′-4-iodobenzyl-N′-methyl)aminoethyl]-5-chloro-2-metho xy-4-(methylamino)benzamide (IMB) was synthesized and labelled with ¹¹C and ¹²⁵I at high specific activities. Both radiotracers were prepared by alkylation reactions with [¹¹C]iodomethane and [¹²⁵I]4-iodobenzyl bromide and appropriate 2° amine precursors. Isolated radiochemical yields of 12-20% for [¹¹C]IMB and 35-50% for [¹²⁵I]IMB were achieved in 24 and 130-150 min respectively. [¹¹C]IMB and [¹²³I]IMB may prove suitable for a direct comparison of PET and SPECT in the localization and quantification of neuroreceptors.

Original language	English (US)
Pages (from-to)	369-373
Number of pages	5
Journal	International Journal of Radiation Applications and Instrumentation. Part
Volume	40
Issue number	5
DOIs	https://doi.org/10.1016/0883-2889(89)90199-8
State	Published - 1989

ASJC Scopus subject areas

Radiation
Engineering(all)

Access to Document

10.1016/0883-2889(89)90199-8

Cite this

@article{be128f4231ee4d17a023271b333f5b19,

title = "Preparation of [11C]- and [125I]IMB: a dopamine D-2 receptor antagonist",

abstract = "A new dopamine D-2 receptor ligand, N-[2-(N′-4-iodobenzyl-N′-methyl)aminoethyl]-5-chloro-2-metho xy-4-(methylamino)benzamide (IMB) was synthesized and labelled with 11C and 125I at high specific activities. Both radiotracers were prepared by alkylation reactions with [11C]iodomethane and [125I]4-iodobenzyl bromide and appropriate 2° amine precursors. Isolated radiochemical yields of 12-20% for [11C]IMB and 35-50% for [125I]IMB were achieved in 24 and 130-150 min respectively. [11C]IMB and [123I]IMB may prove suitable for a direct comparison of PET and SPECT in the localization and quantification of neuroreceptors.",

author = "Wilson, {Alan A.} and Dannals, {Robert F.} and Ravert, {Hayden T.} and Wagner, {Henry N.}",

note = "Funding Information: Acknowledgements--This work was supported in part by USPHS Grant Numbers CA32845 and NS 15080. The authors thank Frederick W. Gilbart for his technical assistance.",

year = "1989",

doi = "10.1016/0883-2889(89)90199-8",

language = "English (US)",

volume = "40",

pages = "369--373",

journal = "International Journal of Radiation Applications and Instrumentation. Part",

issn = "0883-2889",

publisher = "Elsevier Limited",

number = "5",

}

TY - JOUR

T1 - Preparation of [11C]- and [125I]IMB

T2 - a dopamine D-2 receptor antagonist

AU - Wilson, Alan A.

AU - Dannals, Robert F.

AU - Ravert, Hayden T.

AU - Wagner, Henry N.

N1 - Funding Information: Acknowledgements--This work was supported in part by USPHS Grant Numbers CA32845 and NS 15080. The authors thank Frederick W. Gilbart for his technical assistance.

PY - 1989

Y1 - 1989

N2 - A new dopamine D-2 receptor ligand, N-[2-(N′-4-iodobenzyl-N′-methyl)aminoethyl]-5-chloro-2-metho xy-4-(methylamino)benzamide (IMB) was synthesized and labelled with 11C and 125I at high specific activities. Both radiotracers were prepared by alkylation reactions with [11C]iodomethane and [125I]4-iodobenzyl bromide and appropriate 2° amine precursors. Isolated radiochemical yields of 12-20% for [11C]IMB and 35-50% for [125I]IMB were achieved in 24 and 130-150 min respectively. [11C]IMB and [123I]IMB may prove suitable for a direct comparison of PET and SPECT in the localization and quantification of neuroreceptors.

AB - A new dopamine D-2 receptor ligand, N-[2-(N′-4-iodobenzyl-N′-methyl)aminoethyl]-5-chloro-2-metho xy-4-(methylamino)benzamide (IMB) was synthesized and labelled with 11C and 125I at high specific activities. Both radiotracers were prepared by alkylation reactions with [11C]iodomethane and [125I]4-iodobenzyl bromide and appropriate 2° amine precursors. Isolated radiochemical yields of 12-20% for [11C]IMB and 35-50% for [125I]IMB were achieved in 24 and 130-150 min respectively. [11C]IMB and [123I]IMB may prove suitable for a direct comparison of PET and SPECT in the localization and quantification of neuroreceptors.

UR - http://www.scopus.com/inward/record.url?scp=0024475342&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0024475342&partnerID=8YFLogxK

U2 - 10.1016/0883-2889(89)90199-8

DO - 10.1016/0883-2889(89)90199-8

M3 - Article

C2 - 2548972

AN - SCOPUS:0024475342

SN - 0883-2889

VL - 40

SP - 369

EP - 373

JO - International Journal of Radiation Applications and Instrumentation. Part

JF - International Journal of Radiation Applications and Instrumentation. Part

IS - 5

ER -

Preparation of [¹¹C]- and [¹²⁵I]IMB: a dopamine D-2 receptor antagonist

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this