Horti AG, Koren AO, Lee KS, Mukhin AG, Vaupel DB, Kimes AS, Stratton M, London ED. Radiosynthesis and preliminary evaluation of 5-[123/125I]iodo-3-(2(S)-azetidinylmethoxy)pyridine: a radioligand for nicotinic acetylcholine receptors. Nucl Med Biol. 1999; 26(2):175-182.
Musachio JL, Villemagne VL, Scheffel UA, Dannals RF, Dogan AS, Yokoi F, Wong DF. Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon. Nucl Med Biol. 1999; 26(2):201-207.
Specific activity reported: 320 GBq/μmol
In vitro analysis:
Saji H, Ogawa M, Ueda M, Iida Y, Magata Y, Tominaga A, Kawashima H, Kitamura Y, Nakagawa M, Kiyono Y, et al. Evaluation of radioiodinated 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine as a ligand for SPECT investigations of brain nicotinic acetylcholine receptors. Ann Nucl Med. 2002; 16(3):189-200.
Sullivan JP, Donnelly-Roberts D, Briggs CA, Anderson DJ, Gopalakrishnan M, Piattoni-Kaplan M, Campbell JE, McKenna DG, Molinari E, Hettinger AM, et al. A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand. Neuropharmacology. 1996; 35(6):725-734.
Horti AG, Koren AO, Lee KS, Mukhin AG, Vaupel DB, Kimes AS, Stratton M, London ED. Radiosynthesis and preliminary evaluation of 5-[123/125I]iodo-3-(2(S)-azetidinylmethoxy)pyridine: a radioligand for nicotinic acetylcholine receptors. Nucl Med Biol. 1999; 26(2):175-182.
Animal Studies:
Musachio JL, Villemagne VL, Scheffel UA, Dannals RF, Dogan AS, Yokoi F, Wong DF. Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon. Nucl Med Biol. 1999; 26(2):201-207.
Saji H, Ogawa M, Ueda M, Iida Y, Magata Y, Tominaga A, Kawashima H, Kitamura Y, Nakagawa M, Kiyono Y, et al. Evaluation of radioiodinated 5-iodo-3-(2(S)-azetidinylmethoxy)pyridine as a ligand for SPECT investigations of brain nicotinic acetylcholine receptors. Ann Nucl Med. 2002; 16(3):189-200.
Vaupel DB, Mukhin AG, Kimes AS, Horti AG, Koren AO, London ED. In vivo studies with [125I]5-I-A-85380, a nicotinic acetylcholine receptor radioligand. Neuroreport. 1998; 9(10):2311-2317.
Chefer SI, Horti AG, Lee KS, Koren AO, Jones DW, Gorey JG, Links JM, Mukhin AG, Weinberger DR, London ED. In vivo imaging of brain nicotinic acetylcholine receptors with 5-[123I]iodo-A-85380 using single photon emission computed tomography. Life Sci. 1998; 63(25):PL355-PL360.
Fujita M, Tamagnan G, Zoghbi SS...
Clinical Studies:
Ueda M, Iida Y, Mukai T, Mamede M, Ishizu K, Ogawa M, Magata Y, Konishi J, Saji H. 5-[123I]Iodo-A-85380: assessment of pharmacological safety, radiation dosimetry and SPECT imaging of brain nicotinic receptors in healthy human subjects. Ann Nucl Med. 2004; 18(4):337-344
Fujita M, Seibyl JP, Vaupel DB, Tamagnan G, Early M, Zoghbi SS, Baldwin RM, Horti AG, Kore NA, Mukhin AG, et al. Whole-body biodistribution, radiation absorbed dose, and brain SPET imaging with [123i]5-i-A-85380 in healthy human subjects. Eur J Nucl Med Mol Imaging. 2002; 29(2):183-190.
Mamede M, Ishizu K, Ueda M, Mukai T, Iida Y, Fukuyama H, Saga T, Saji H. Quantification of human nicotinic acetylcholine receptors with 123I-5IA SPECT. J Nucl Med. 2004; 45(9):1458-1470.