6-[18F]Fluoro-A-85380: an in vivo tracer for the nicotinic acetylcholine receptor - PubMed (original) (raw)
6-[18F]Fluoro-A-85380: an in vivo tracer for the nicotinic acetylcholine receptor
U Scheffel et al. Nucl Med Biol. 2000 Jan.
Free article
Abstract
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.
Similar articles
- 2-[18F]Fluoro-A-85380, an in vivo tracer for the nicotinic acetylcholine receptors.
Horti AG, Scheffel U, Koren AO, Ravert HT, Mathews WB, Musachio JL, Finley PA, London ED, Dannals RF. Horti AG, et al. Nucl Med Biol. 1998 Oct;25(7):599-603. doi: 10.1016/s0969-8051(98)00031-6. Nucl Med Biol. 1998. PMID: 9804040 - Synthesis and nicotinic acetylcholine receptor in vivo binding properties of 2-fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine: a new positron emission tomography ligand for nicotinic receptors.
Doll F, Dolci L, Valette H, Hinnen F, Vaufrey F, Guenther I, Fuseau C, Coulon C, Bottlaender M, Crouzel C. Doll F, et al. J Med Chem. 1999 Jun 17;42(12):2251-9. doi: 10.1021/jm9910223. J Med Chem. 1999. PMID: 10377231 - 6-[18F]fluoro-A-85380, a novel radioligand for in vivo imaging of central nicotinic acetylcholine receptors.
Horti AG, Chefer SI, Mukhin AG, Koren AO, Gündisch D, Links JM, Kurian V, Dannals RF, London ED. Horti AG, et al. Life Sci. 2000 Jun 16;67(4):463-9. doi: 10.1016/s0024-3205(00)00635-4. Life Sci. 2000. PMID: 11003056 - Central in vivo nicotinic acetylcholine receptor imaging agents for positron emission tomography (PET) and single photon emission computed tomography (SPECT).
Ogawa M, Tsukada H, Hatano K, Ouchi Y, Saji H, Magata Y. Ogawa M, et al. Biol Pharm Bull. 2009 Mar;32(3):337-40. doi: 10.1248/bpb.32.337. Biol Pharm Bull. 2009. PMID: 19252274 Review. - 2-[18F]Fluoro-3-[2(S)-2-azetidinylmethoxy]pyridine.
Leung K. Leung K. 2006 Jun 23 [updated 2008 Apr 8]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2006 Jun 23 [updated 2008 Apr 8]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 20641602 Free Books & Documents. Review.
Cited by
- Beta-amyloid activates the mitogen-activated protein kinase cascade via hippocampal alpha7 nicotinic acetylcholine receptors: In vitro and in vivo mechanisms related to Alzheimer's disease.
Dineley KT, Westerman M, Bui D, Bell K, Ashe KH, Sweatt JD. Dineley KT, et al. J Neurosci. 2001 Jun 15;21(12):4125-33. doi: 10.1523/JNEUROSCI.21-12-04125.2001. J Neurosci. 2001. PMID: 11404397 Free PMC article. - Development of radioligands with optimized imaging properties for quantification of nicotinic acetylcholine receptors by positron emission tomography.
Horti AG, Gao Y, Kuwabara H, Dannals RF. Horti AG, et al. Life Sci. 2010 Apr 10;86(15-16):575-84. doi: 10.1016/j.lfs.2009.02.029. Epub 2009 Mar 18. Life Sci. 2010. PMID: 19303028 Free PMC article. Review. - Single photon emission computed tomography experience with (S)-5-[(123)I]iodo-3-(2-azetidinylmethoxy)pyridine in the living human brain of smokers and nonsmokers.
Brasić JR, Zhou Y, Musachio JL, Hilton J, Fan H, Crabb A, Endres CJ, Reinhardt MJ, Dogan AS, Alexander M, Rousset O, Maris MA, Galecki J, Nandi A, Wong DF. Brasić JR, et al. Synapse. 2009 Apr;63(4):339-58. doi: 10.1002/syn.20611. Synapse. 2009. PMID: 19140167 Free PMC article. Clinical Trial. - Clinical Perspective and Recent Development of PET Radioligands for Imaging Cerebral Nicotinic Acetylcholine Receptors.
Horti AG, Wong DF. Horti AG, et al. PET Clin. 2009 Jan 1;4(1):89-100. doi: 10.1016/j.cpet.2009.04.014. PET Clin. 2009. PMID: 20046884 Free PMC article. No abstract available.