pubmed-article:8176704 | rdf:type | pubmed:Citation | lld:pubmed |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C0034721 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C0034693 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C0010097 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C0162512 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C0016733 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C0205145 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C0013030 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C0028823 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C0220781 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C1167622 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C1883254 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C1159719 | lld:lifeskim |
pubmed-article:8176704 | lifeskim:mentions | umls-concept:C1510827 | lld:lifeskim |
pubmed-article:8176704 | pubmed:issue | 9 | lld:pubmed |
pubmed-article:8176704 | pubmed:dateCreated | 1994-6-9 | lld:pubmed |
pubmed-article:8176704 | pubmed:abstractText | A novel entry to tropane analogs of cocaine was developed on the basis of the reaction of rhodium-stabilized vinylcarbenoids with pyrroles. These analogs were tested in binding to dopamine and serotonin (5-HT) transporters in membranes from rat striatum and frontal cortex. In all the analogs, the aryl group at the 3-position was directly bound to the tropane ring (as in WIN-35,428), and methyl or ethyl ketone moieties were present at the 2-position instead of the typical ester group. The series of analogs containing a 2-naphthyl group at the 3-position were most potent, with Ki values < 1 nM in binding to both dopamine and 5-HT transporters. Although the unsubstituted 2-naphthyl analog was nonselective at dopamine and 5-HT transport sites, other compounds were selective for either site. In general, compounds with relatively small substituents on the aromatic moiety (such as p-methyl or p-fluoro) were relatively selective for the dopamine transporters, while a p-isopropylphenyl derivative was selective for the 5-HT transport sites. This latter compound represents the first N-methyltropane derivative specific for 5-HT transporters. Resolution of two of the most significant analogs was achieved by HPLC on a chiral stationary phase; the active enantiomer of a 2-naphthyl analog exhibited Ki values of < 0.1 nM at both dopamine and 5-HT transporter sites. | lld:pubmed |
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pubmed-article:8176704 | pubmed:language | eng | lld:pubmed |
pubmed-article:8176704 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8176704 | pubmed:citationSubset | IM | lld:pubmed |
pubmed-article:8176704 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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pubmed-article:8176704 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8176704 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8176704 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8176704 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8176704 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8176704 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8176704 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8176704 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
pubmed-article:8176704 | pubmed:status | MEDLINE | lld:pubmed |
pubmed-article:8176704 | pubmed:month | Apr | lld:pubmed |
pubmed-article:8176704 | pubmed:issn | 0022-2623 | lld:pubmed |
pubmed-article:8176704 | pubmed:author | pubmed-author:ChildersS RSR | lld:pubmed |
pubmed-article:8176704 | pubmed:author | pubmed-author:SextonTT | lld:pubmed |
pubmed-article:8176704 | pubmed:author | pubmed-author:HubyN JNJ | lld:pubmed |
pubmed-article:8176704 | pubmed:author | pubmed-author:DaviesH MHM | lld:pubmed |
pubmed-article:8176704 | pubmed:author | pubmed-author:SaikaliEE | lld:pubmed |
pubmed-article:8176704 | pubmed:author | pubmed-author:GilliattV JVJ | lld:pubmed |
pubmed-article:8176704 | pubmed:author | pubmed-author:MatasiJ JJJ | lld:pubmed |
pubmed-article:8176704 | pubmed:issnType | Print | lld:pubmed |
pubmed-article:8176704 | pubmed:day | 29 | lld:pubmed |
pubmed-article:8176704 | pubmed:volume | 37 | lld:pubmed |
pubmed-article:8176704 | pubmed:owner | NLM | lld:pubmed |
pubmed-article:8176704 | pubmed:authorsComplete | Y | lld:pubmed |
pubmed-article:8176704 | pubmed:pagination | 1262-8 | lld:pubmed |
pubmed-article:8176704 | pubmed:dateRevised | 2007-11-14 | lld:pubmed |
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pubmed-article:8176704 | pubmed:year | 1994 | lld:pubmed |
pubmed-article:8176704 | pubmed:articleTitle | Synthesis of 2 beta-acyl-3 beta-aryl-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites in rat striatum and frontal cortex. | lld:pubmed |
pubmed-article:8176704 | pubmed:affiliation | Department of Chemistry, Wake Forest University, Winston-Salem, North Carolina 27109. | lld:pubmed |
pubmed-article:8176704 | pubmed:publicationType | Journal Article | lld:pubmed |
pubmed-article:8176704 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
pubmed-article:8176704 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
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