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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6
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pubmed:dateCreated |
1996-2-8
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pubmed:abstractText |
The tritiated dopamine reuptake inhibitor [3H]NNC 12-0781 ([1-[2-(bis(4-fluorophenyl)-methoxy)-ethyl]-4-(3-(2-furanyl)-2,3-[3H] - propyl)-piperazine) was radiolabelled in one step starting from 1-[2-(bis(4-fluorophenyl)-methoxy)-ethyl]-4-(3-(2-furanyl)-2-propenyl)- piperazine, using tritium gas and PdO as catalyst. The radiochemical purity of [3H]NNC 12-0781 was higher than 99% after HPLC purification with a specific radioactivity of 21 Ci/mmol. [3H]NNC 12-0781 bound specifically to rat striatum in vitro at +4 degrees C with a Kd of 1.76 nM and Bmax of 587 fmol/mg tissue. The nonspecific binding was about 10% at Kd. At +37 degrees C no acceptable binding was observed. The association of [3H]NNC 12-0781 thus has the characteristics of a radioligand for the dopamine transporter in vitro at +4 degrees C.
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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 |
Aug
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pubmed:issn |
0969-8051
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
22
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
711-7
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:8535331-Animals,
pubmed-meshheading:8535331-Brain,
pubmed-meshheading:8535331-Carrier Proteins,
pubmed-meshheading:8535331-Cell Membrane,
pubmed-meshheading:8535331-Chromatography, High Pressure Liquid,
pubmed-meshheading:8535331-Corpus Striatum,
pubmed-meshheading:8535331-Dopamine Plasma Membrane Transport Proteins,
pubmed-meshheading:8535331-Dopamine Uptake Inhibitors,
pubmed-meshheading:8535331-Isotope Labeling,
pubmed-meshheading:8535331-Kinetics,
pubmed-meshheading:8535331-Male,
pubmed-meshheading:8535331-Membrane Glycoproteins,
pubmed-meshheading:8535331-Membrane Transport Proteins,
pubmed-meshheading:8535331-Nerve Tissue Proteins,
pubmed-meshheading:8535331-Piperazines,
pubmed-meshheading:8535331-Radioligand Assay,
pubmed-meshheading:8535331-Rats,
pubmed-meshheading:8535331-Rats, Wistar,
pubmed-meshheading:8535331-Tritium
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pubmed:year |
1995
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pubmed:articleTitle |
Synthesis and binding properties of [3H]NNC 12-0781, a new radioligand for the dopamine reuptake system.
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pubmed:affiliation |
Novo Nordisk A/S, Pharmaceuticals Division, Maaloev, Denmark.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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