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

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...

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Veröffentlicht in:	Nuclear medicine and biology 1998-10, Vol.25 (7), p.599-603
Hauptverfasser:	Horti, Andrew G, Scheffel, Ursula, Koren, Andrei O, Ravert, Hayden T, Mathews, William B, Musachio, John L, Finley, Paige A, London, Edythe D, Dannals, Robert F
Format:	Artikel
Sprache:	eng
Schlagworte:	A-85380 derivative Acetylcholine receptor Animals Azetidines - metabolism Azetidines - pharmacokinetics Azetidines - toxicity Binding, Competitive - drug effects Biological and medical sciences Brain distribution Contrast media. Radiopharmaceuticals Fluorine Radioisotopes Injections, Intravenous Male Medical sciences Mice Nicotinic receptor PET Pharmacology Pharmacology. Drug treatments Radiotracer Receptors, Nicotinic - analysis Receptors, Nicotinic - metabolism Tissue Distribution
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Zusammenfassung:	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.
ISSN:	0969-8051 1872-9614
DOI:	10.1016/S0969-8051(98)00031-6