Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Brain / metabolism*
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Carrier Proteins / metabolism
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Cell Membrane / metabolism
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Chromatography, High Pressure Liquid
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Corpus Striatum / metabolism
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Dopamine Plasma Membrane Transport Proteins
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Dopamine Uptake Inhibitors / chemical synthesis
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Dopamine Uptake Inhibitors / metabolism*
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Isotope Labeling / methods
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Kinetics
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Male
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Membrane Glycoproteins*
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Membrane Transport Proteins*
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Nerve Tissue Proteins*
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Piperazines / chemical synthesis*
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Piperazines / metabolism*
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Piperazines / pharmacokinetics
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Radioligand Assay / methods
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Rats
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Rats, Wistar
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Tritium
Substances
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Carrier Proteins
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Dopamine Plasma Membrane Transport Proteins
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Dopamine Uptake Inhibitors
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Membrane Glycoproteins
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Membrane Transport Proteins
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NNC 12-0781
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Nerve Tissue Proteins
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Piperazines
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Tritium