| pubmed-article:18605717 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C0011923 | lld:lifeskim |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C0228174 | lld:lifeskim |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C0034830 | lld:lifeskim |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C0019225 | lld:lifeskim |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C0032743 | lld:lifeskim |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C1527121 | lld:lifeskim |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C1880355 | lld:lifeskim |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C2698651 | lld:lifeskim |
| pubmed-article:18605717 | lifeskim:mentions | umls-concept:C0871161 | lld:lifeskim |
| pubmed-article:18605717 | pubmed:issue | 15 | lld:pubmed |
| pubmed-article:18605717 | pubmed:dateCreated | 2008-8-7 | lld:pubmed |
| pubmed-article:18605717 | pubmed:abstractText | Several isomers of 7-methyl-2-exo-([(18)F]fluoropyridinyl-5'-pyridinyl)-7-azabicyclo[2.2.1]heptane have been developed as radioligands with optimized brain kinetics for PET imaging of nAChR. The binding assay demonstrated that all isomers are beta-nAChR selective ligands with Ki = 0.02-0.3 nM. The experimental lipophilicity values of all isomers were in the optimal range for the cerebral radioligands (log D7.4= 0.67-0.99). The isomers with higher binding affinity manifested slow baboon brain kinetics, whereas the isomer with the lowest binding affinity (Ki = 0.3 nM) ((-)-7-methyl-2- exo-[3'-(6-[(18)F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, [(18)F](-)-6c) and greatest lipophilicity (log D 7.4 = 0.99) exhibited optimal brain kinetics. [(18)F](-)-6c manifests a unique combination of the optimally rapid brain kinetics, high BP and brain uptake, and favorable metabolic profile. Pharmacological studies showed that (-)-6c is an alpha4beta2-nAChR antagonist with low side effects in mice. This combination of imaging properties suggests that [(18)F]-(-)- 6c is a potentially superior replacement for 2-[(18)F]fluoro-A-85380 and 6-[(18)F]fluoro-A-85380, the only available nAChR PET radioligands for humans. | lld:pubmed |
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| pubmed-article:18605717 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18605717 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18605717 | pubmed:language | eng | lld:pubmed |
| pubmed-article:18605717 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18605717 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:18605717 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18605717 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18605717 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18605717 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18605717 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:18605717 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:18605717 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:18605717 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:18605717 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:WongDean FDF | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:RavertHayden... | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:DannalsRobert... | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:XiaoYingxianY | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:HortiAndrew... | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:KumarAnilA | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:KuwabaraHirot... | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:HiltonJohnJ | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:SpivakCharles... | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:GaoYongjunY | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:AlexanderMoha... | lld:pubmed |
| pubmed-article:18605717 | pubmed:author | pubmed-author:KellarKenneth... | lld:pubmed |
| pubmed-article:18605717 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:18605717 | pubmed:day | 14 | lld:pubmed |
| pubmed-article:18605717 | pubmed:volume | 51 | lld:pubmed |
| pubmed-article:18605717 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:18605717 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:18605717 | pubmed:pagination | 4751-64 | lld:pubmed |
| pubmed-article:18605717 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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| pubmed-article:18605717 | pubmed:year | 2008 | lld:pubmed |
| pubmed-article:18605717 | pubmed:articleTitle | Discovery of (-)-7-methyl-2-exo-[3'-(6-[18F]fluoropyridin-2-yl)-5'-pyridinyl]-7-azabicyclo[2.2.1]heptane, a radiolabeled antagonist for cerebral nicotinic acetylcholine receptor (alpha4beta2-nAChR) with optimal positron emission tomography imaging properties. | lld:pubmed |
| pubmed-article:18605717 | pubmed:affiliation | Department of Radiology, Division of Nuclear Medicine, The Johns Hopkins UniVersity School of Medicine, 600 North Wolfe Street, Baltimore, Maryland 21287-0816, USA. | lld:pubmed |
| pubmed-article:18605717 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:18605717 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| pubmed-article:18605717 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:18605717 | lld:chembl |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:18605717 | lld:pubmed |
