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Uptake of the dopaminergic neurotoxin, norsalsolinol, into PC12 cells via dopamine transporter.

Abstract
The uptake of norsalsolinol, a neurotoxin candidate causing parkinsonism-like symptoms, was studied in PC12 cells. The compound was actively taken up by the PC12 cells, with a Km value of 176.24 +/-9.1 microM and a maximum velocity of 55.6 +/- 7.0 pmol/min per mg protein; norsalsolinol uptake was dependent on the presence of extracellular Na+. The uptake of norsalsolinol was sensitive to two dopamine transporter inhibitors, GBR-12909 and reserpine, but was less sensitive to desipramine, a noradrenaline transporter inhibitor. Dopamine competitively inhibited norsalsolinol uptake into PC12 cells with a Ki value of 271.2 +/- 61.6 microM. These results suggest that norsalsolinol is taken up into PC12 cells mainly by the dopamine transporter.
AuthorsY Maruyama, Y Suzuki, A Kazusaka, S Fujita
JournalArchives of toxicology (Arch Toxicol) Vol. 75 Issue 4 Pg. 209-13 (Jun 2001) ISSN: 0340-5761 [Print] Germany
PMID11482518 (Publication Type: Journal Article)
Chemical References
  • Adrenergic Uptake Inhibitors
  • Dopamine Plasma Membrane Transport Proteins
  • Dopamine Uptake Inhibitors
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • Piperazines
  • Salsoline Alkaloids
  • Reserpine
  • vanoxerine
  • norsalsolinol
  • Desipramine
  • Dopamine
Topics
  • Adrenergic Uptake Inhibitors (pharmacology)
  • Animals
  • Cells, Cultured
  • Chromatography, High Pressure Liquid
  • Desipramine (pharmacology)
  • Dopamine (metabolism)
  • Dopamine Plasma Membrane Transport Proteins
  • Dopamine Uptake Inhibitors (pharmacology)
  • Dose-Response Relationship, Drug
  • Membrane Glycoproteins
  • Membrane Transport Proteins (metabolism)
  • Nerve Tissue Proteins
  • PC12 Cells
  • Piperazines (pharmacology)
  • Rats
  • Reserpine (pharmacology)
  • Reverse Transcriptase Polymerase Chain Reaction
  • Salsoline Alkaloids (metabolism, toxicity)

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