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

Precision Radiotheranostics Translation Center (PRTC)

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

64 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
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

Keywords

Iodine-123
Nicotinic acetylcholine receptor
SPECT

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10.1016/S0969-8051(98)00101-2

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@article{b43305c4c92c4767a589ab81340406ba,

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",

volume = "26",

pages = "201--207",

journal = "Nuclear Medicine and Biology",

issn = "0969-8051",

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

UR - https://www.scopus.com/pages/publications/0033019826

U2 - 10.1016/S0969-8051(98)00101-2

DO - 10.1016/S0969-8051(98)00101-2

M3 - Article

C2 - 10100220

AN - SCOPUS:0033019826

SN - 0969-8051

VL - 26

SP - 201

EP - 207

JO - Nuclear Medicine and Biology

JF - Nuclear Medicine and Biology

IS - 2

ER -

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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