6-[18F]Fluoro-A-85380: an in vivo tracer for the nicotinic acetylcholine receptor.
6-[18F]Fluoro-3-(2(S)-azetidinylmethoxy)pyridine (6-[18F]fluoro-A-85380 or 6-[18F]FA), a new tracer for positron emission tomography, was synthesized by no-carrier-added [18F] fluorination of 6-iodo-3-((1-tert-butoxycarbonyl-2(S)-azetidinyl)methoxy)pyridine followed by acidic deprotection. 6-[18F]FA followed the regional densities of brain nicotinic acetylcholine receptors (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 6-FA. A preliminary toxicology study of the 6-FA showed a relatively low biological effect.
Scheffel
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U
Division of Nuclear Medicine and Radiation Health Sciences, The Johns Hopkins Medical Institutions, Baltimore, Maryland 21205-2179, USA.
Horti
A G
AG
Koren
A O
AO
Ravert
H T
HT
Banta
J P
JP
Finley
P A
PA
London
E D
ED
Dannals
R F
RF
D000818:Animals; D001384:Azetidines / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics*; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D005462:Fluorine Radioisotopes; D007279:Injections, Subcutaneous; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D011854:Radiochemistry; D011978:Receptors, Nicotinic / Q000378:metabolism*; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed
C104288:A 85380; D001384:Azetidines; D005462:Fluorine Radioisotopes; D011978:Receptors, Nicotinic