Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon

John L. Musachio; Victor L. Villemagne; Ursula A. Scheffel; Robert F. Dannals; A. Semih Dogan; Fuji Yokoi; Dean F. Wong

doi:10.1016/S0969-8051(98)00101-2

Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon

John L. Musachio, Victor L. Villemagne, Ursula A. Scheffel, Robert F. Dannals, A. Semih Dogan, Fuji Yokoi, Dean F. Wong

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

62 Scopus citations

Abstract

A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (S)-5-[¹²³I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-1A, has been developed. The two-step sequence produced [¹²³I]-5-1A in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (>8,500 mCi/μmol). Preliminary single photon emission computed tomography studies with [¹²³I]-5-1A in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [¹²³I]-5-1A uptake in all brain regions (78-59% reduction), demonstrating the specificity of the radiotracer.

Original language	English (US)
Pages (from-to)	201-207
Number of pages	7
Journal	Nuclear Medicine and Biology
Volume	26
Issue number	2
DOIs	https://doi.org/10.1016/S0969-8051(98)00101-2
State	Published - Feb 1999
Externally published	Yes

Keywords

Iodine-123
Nicotinic acetylcholine receptor
SPECT

ASJC Scopus subject areas

Molecular Medicine
Radiology Nuclear Medicine and imaging
Cancer Research

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10.1016/S0969-8051(98)00101-2

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title = "Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon",

abstract = "A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (S)-5-[123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-1A, has been developed. The two-step sequence produced [123I]-5-1A in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (>8,500 mCi/μmol). Preliminary single photon emission computed tomography studies with [123I]-5-1A in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [123I]-5-1A uptake in all brain regions (78-59% reduction), demonstrating the specificity of the radiotracer.",

keywords = "Iodine-123, Nicotinic acetylcholine receptor, SPECT",

author = "Musachio, {John L.} and Villemagne, {Victor L.} and Scheffel, {Ursula A.} and Dannals, {Robert F.} and Dogan, {A. Semih} and Fuji Yokoi and Wong, {Dean F.}",

note = "Funding Information: This work was supported by USPHS grant NCI CA 77349 (J. L. M.) and HD 24448 (D. F. W.). The NMR facility was established by USPHS grants GM 27512 and 1S10-RR06262. We thank Dr. Yougen Zhan, Dr. T. K. Natarajan, Richard Gilbert, CNMT, and Paige Finley for their technical assistance. ",

year = "1999",

month = feb,

doi = "10.1016/S0969-8051(98)00101-2",

language = "English (US)",

volume = "26",

pages = "201--207",

journal = "International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology",

issn = "0969-8051",

publisher = "Elsevier Inc.",

number = "2",

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T1 - Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon

AU - Musachio, John L.

AU - Villemagne, Victor L.

AU - Scheffel, Ursula A.

AU - Dannals, Robert F.

AU - Dogan, A. Semih

AU - Yokoi, Fuji

AU - Wong, Dean F.

N1 - Funding Information: This work was supported by USPHS grant NCI CA 77349 (J. L. M.) and HD 24448 (D. F. W.). The NMR facility was established by USPHS grants GM 27512 and 1S10-RR06262. We thank Dr. Yougen Zhan, Dr. T. K. Natarajan, Richard Gilbert, CNMT, and Paige Finley for their technical assistance.

PY - 1999/2

Y1 - 1999/2

N2 - A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (S)-5-[123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-1A, has been developed. The two-step sequence produced [123I]-5-1A in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (>8,500 mCi/μmol). Preliminary single photon emission computed tomography studies with [123I]-5-1A in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [123I]-5-1A uptake in all brain regions (78-59% reduction), demonstrating the specificity of the radiotracer.

AB - A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (S)-5-[123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-1A, has been developed. The two-step sequence produced [123I]-5-1A in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (>8,500 mCi/μmol). Preliminary single photon emission computed tomography studies with [123I]-5-1A in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [123I]-5-1A uptake in all brain regions (78-59% reduction), demonstrating the specificity of the radiotracer.

KW - Iodine-123

KW - Nicotinic acetylcholine receptor

KW - SPECT

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Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon

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Keywords

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