Nuclear medicine and biology, 2001-11, Vol.28 (8), p.911-921
2001
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Details
- Autor(en) / Beteiligte
- Titel
- [125/123I] 5-iodo-3-pyridyl ethers: syntheses and binding to neuronal nicotinic acetylcholine receptors
- Ist Teil von
- Nuclear medicine and biology, 2001-11, Vol.28 (8), p.911-921
- Ort / Verlag
- Amsterdam: Elsevier
- Erscheinungsjahr
- 2001
- Quelle
- Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)
- Beschreibungen/Notizen
- 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 (thalamus > frontal cortex > cerebellum) and a more rapid pharmacokinetic profile relative to azetidinyl 3-pyridyl ether based ligands.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0969-8051eISSN: 1872-9614DOI: 10.1016/S0969-8051(01)00258-XTitel-ID: cdi_proquest_miscellaneous_72278932
- Format
- –
- Schlagworte
- Animals, Biological and medical sciences, Brain - diagnostic imaging, Contrast media. Radiopharmaceuticals, Ethers - chemical synthesis, Ethers - metabolism, Ethers - pharmacokinetics, Investigative techniques, diagnostic techniques (general aspects), Male, Medical sciences, Mice, Nervous system, Papio, Pharmacology. Drug treatments, Pyridines - chemical synthesis, Pyridines - metabolism, Pyridines - pharmacokinetics, Radionuclide investigations, Receptors, Nicotinic - metabolism, Tissue Distribution, Tomography, Emission-Computed, Single-Photon