Paraxanthine displaces the binding of [3H]SCH 23390 from rat striatal membranes

Sergi Ferré, Teresa Guix, Joan Sallés, Albert Badia, Pilar Parra, Francesc Jané, Mario Herrera-Marschitz, Urban Ungerstedt, Miquel Casas

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Abstract

We present evidence showing that paraxanthine (1,7-dimethylxanthine), the main metabolite of caffeine in man, displaces the binding of [3H]SCH 23390, a radioligand which selectively labels dopamine D-1 receptors when used at low concentrations, from striatal membranes of the rat. The displacement was competitive and indicated the existence of two affinity states (Hill coefficient = 0.49; K(high) = 0.15 μM; K(low) = 95.9 μM, %R(high) = 32.4). When the stable GTP analog Gpp(NH)p was included, the displacement curve indicated the presence of only the low-affinity state (Hill coefficient = 1.16; Ki = 72.1 μM). However, paraxanthine did not displace the specific binding of [3H]spiperone. After injection of 30 mg/kg s.c. of caffeine, a maximum of 10 μM of paraxanthine was found in striatal homogenates, which could be sufficient to occupy dopamine D-1 receptors. Our results suggest that a dopaminergic action of paraxanthine could be involved in the behavioral stimulation produced by caffeine. © 1990.
Original languageEnglish
Pages (from-to)295-299
JournalEuropean Journal of Pharmacology
Volume179
Issue number3
DOIs
Publication statusPublished - 25 Apr 1990

Keywords

  • Dopamine D-1 receptors
  • Methylxanthines
  • Paraxanthine
  • Striatum
  • [ H]SCH 23390 3

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    Ferré, S., Guix, T., Sallés, J., Badia, A., Parra, P., Jané, F., Herrera-Marschitz, M., Ungerstedt, U., & Casas, M. (1990). Paraxanthine displaces the binding of [3H]SCH 23390 from rat striatal membranes. European Journal of Pharmacology, 179(3), 295-299. https://doi.org/10.1016/0014-2999(90)90168-6