2-[18F]fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors

Andrew G. Horti; Ursula Scheffel; Andrei O. Koren; Hayden T Ravert; William B. Mathews; John L. Musachio; Paige A. Finley; Edythe D. London; Robert F. Dannals

doi:10.1016/S0969-8051(98)00031-6

2-[¹⁸F]fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors

Andrew G. Horti, Ursula Scheffel, Andrei O. Koren, Hayden T Ravert, William B. Mathews, John L. Musachio, Paige A. Finley, Edythe D. London, Robert F. Dannals

School of Medicine

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

76 Scopus citations

Abstract

The in vivo brain regional distribution of 2-[¹⁸F]fluoro-A-85380, a novel tracer for positron emission tomographic (PET) studies, followed the regional densities of brain nAChRs reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 2-fluoro-A-85380. A preliminary toxicology study of the 2-fluoro- A-85380 showed a relatively low biological effect. 2-[¹⁸F]Fluoro-A-85380 holds promise as a useful radiotracer for imaging of nAChRs with PET.

Original language	English (US)
Pages (from-to)	599-603
Number of pages	5
Journal	Nuclear Medicine and Biology
Volume	25
Issue number	7
DOIs	https://doi.org/10.1016/S0969-8051(98)00031-6
State	Published - Oct 1998

Keywords

A-85380 derivative
Acetylcholine receptor
Brain distribution
Nicotinic receptor
PET
Pharmacology
Radiotracer

ASJC Scopus subject areas

Molecular Medicine
Radiology Nuclear Medicine and imaging
Cancer Research

Access to Document

10.1016/S0969-8051(98)00031-6

Cite this

@article{bd946475304a442db22cabaf4dbd9026,

title = "2-[18F]fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors",

abstract = "The in vivo brain regional distribution of 2-[18F]fluoro-A-85380, a novel tracer for positron emission tomographic (PET) studies, followed the regional densities of brain nAChRs reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 2-fluoro-A-85380. A preliminary toxicology study of the 2-fluoro- A-85380 showed a relatively low biological effect. 2-[18F]Fluoro-A-85380 holds promise as a useful radiotracer for imaging of nAChRs with PET.",

keywords = "A-85380 derivative, Acetylcholine receptor, Brain distribution, Nicotinic receptor, PET, Pharmacology, Radiotracer",

author = "Horti, {Andrew G.} and Ursula Scheffel and Koren, {Andrei O.} and Ravert, {Hayden T} and Mathews, {William B.} and Musachio, {John L.} and Finley, {Paige A.} and London, {Edythe D.} and Dannals, {Robert F.}",

year = "1998",

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doi = "10.1016/S0969-8051(98)00031-6",

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T1 - 2-[18F]fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors

AU - Horti, Andrew G.

AU - Scheffel, Ursula

AU - Koren, Andrei O.

AU - Ravert, Hayden T

AU - Mathews, William B.

AU - Musachio, John L.

AU - Finley, Paige A.

AU - London, Edythe D.

AU - Dannals, Robert F.

PY - 1998/10

Y1 - 1998/10

N2 - The in vivo brain regional distribution of 2-[18F]fluoro-A-85380, a novel tracer for positron emission tomographic (PET) studies, followed the regional densities of brain nAChRs reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 2-fluoro-A-85380. A preliminary toxicology study of the 2-fluoro- A-85380 showed a relatively low biological effect. 2-[18F]Fluoro-A-85380 holds promise as a useful radiotracer for imaging of nAChRs with PET.

AB - The in vivo brain regional distribution of 2-[18F]fluoro-A-85380, a novel tracer for positron emission tomographic (PET) studies, followed the regional densities of brain nAChRs reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 2-fluoro-A-85380. A preliminary toxicology study of the 2-fluoro- A-85380 showed a relatively low biological effect. 2-[18F]Fluoro-A-85380 holds promise as a useful radiotracer for imaging of nAChRs with PET.

KW - A-85380 derivative

KW - Acetylcholine receptor

KW - Brain distribution

KW - Nicotinic receptor

KW - PET

KW - Pharmacology

KW - Radiotracer

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