[125/123I] 5-Iodo-3-pyridyl ethers. syntheses and binding to neuronal nicotinic acetylcholine receptors

Autor:	H, Fan, U A, Scheffel, P, Rauseo, Y, Xiao, A S, Dogan, F, Yokoi, J, Hilton, K J, Kellar, D F, Wong, J L, Musachio
Rok vydání:	2001
Předmět:	Male Tomography Emission-Computed Single-Photon Mice Pyridines Animals Brain Tissue Distribution Receptors Nicotinic Ethers Papio
Zdroj:	Nuclear medicine and biology. 28(8)
ISSN:	0969-8051
Popis:	Three 3-pyridyl ether nicotinic ligands-(S)-5-Iodo-3-[(2-pyrrolidinyl)-methoxy]pyridine (5-iodo-A-85865), (S)-5-Iodo-3-[1-(methyl)-2-pyrrolidinyl-methoxy]pyridine (5-Iodo-A-84543), and (S)-5-iodo-3-[1-methyl-(2-azetidinyl)-methoxy]pyridine (5-iodo-N-Me-A-85380) were labeled with I-125/I-123, and their ability to label high-affinity brain nicotinic acetylcholine receptors (nAChRs) was evaluated. The most promising ligand, [123/125I] 5-iodo-A-85865, showed approximately 65% inhibition of radioactivity uptake in thalamus in mice pretreated with cytisine. Preliminary SPECT imaging studies with [123I] 5-iodo-A-85865 revealed a distribution profile consistent with nAChRs (thalamusfrontal cortexcerebellum) and a more rapid pharmacokinetic profile relative to azetidinyl 3-pyridyl ether based ligands.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=pmid________::704fed3c83e700c86327fc606cee1337 https://pubmed.ncbi.nlm.nih.gov/11711310 Zobrazit plný text záznamu Full Text from ScienceDirect