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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
14
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pubmed:dateCreated |
2008-7-21
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pubmed:abstractText |
We synthesized several novel 2-O- or 11-O-substituted N-alkylnoraporphines and assessed their affinities at dopamine D(1) and D(2), and serotonin 5-HT(1A) receptors in rat forebrain tissue. Tested compounds displayed moderate to high affinities to D(2) receptors but low affinities to D(1) and 5HT(1A) receptors. The findings accord with previous evidence of a lipophilic cavity on the surface of the D(2) receptor to accommodate N-alkyl moieties of aporphines. The most D(2)-potent (K(i)=97 nM) and selective novel agent (>100-fold vs. D(1) and 5-HT(1A) sites) was R(-)-2-(2-hydroxyethoxy)-11-hydroxy-N-n-propylnoraporphine (compound 11).
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3971-3
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pubmed:meshHeading |
pubmed-meshheading:18585036-Animals,
pubmed-meshheading:18585036-Aporphines,
pubmed-meshheading:18585036-Chemistry, Pharmaceutical,
pubmed-meshheading:18585036-Drug Design,
pubmed-meshheading:18585036-Kinetics,
pubmed-meshheading:18585036-Models, Chemical,
pubmed-meshheading:18585036-Prosencephalon,
pubmed-meshheading:18585036-Protein Binding,
pubmed-meshheading:18585036-Rats,
pubmed-meshheading:18585036-Receptor, Serotonin, 5-HT1A,
pubmed-meshheading:18585036-Receptors, Dopamine D1,
pubmed-meshheading:18585036-Receptors, Dopamine D2
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis and binding studies of 2-O- and 11-O-substituted N-alkylnoraporphines.
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pubmed:affiliation |
Alcohol Drug Abuse Research Center and Mailman Research Center, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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