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Radioreceptor binding reveals the potencies of N,N-disubstituted 2-aminotetralins as D2 dopamine agonists

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Summary

The affinity of a series of N,N-disubstituted 2-aminotetralins for the rat striatal D2 dopamine receptor labelled by [3H]spiperone has been determined. Displacement data for the more potent 2-aminotetralins were better described by a model where the compounds competed for [3H]spiperone at two sites. The high affinity component accounted for approximately 80% of the total sites. Displacement curves for all 2-aminotetralins were shifted to the right by 100 μM guanosine-5′-triphosphate; a result attributable to the redistribution of 13–47% of the sites to a low affinity form. These data are consistent with the N,N-disubstituted 2-aminotetralins being agonists at the D2 dopamine receptor. In particular, the affinities of the 5-hydroxy-2-aminotetralins were as high as those of traditional dopamine agonists.

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Author notes

  1. M. Cincotta, D. J. de Vries, P. Tepper, D. Dijkstra & A. S. Horn

    Present address: Laboratory of Cellular Carcinogenesis and Tumour Promotion, National Cancer Institute, 20892, Bethesda, MD, USA

Authors and Affiliations

  1. Clinical Pharmacology and Therapeutics Unit, Austin Hospital, University of Melbourne, 3084, Heidelberg, Victoria, Australia

    P. M. Beart, C. J. Cook, M. Cincotta & D. J. de Vries

  2. Department of Pharmacy, University of Groningen, 2 Antonius Deusinglaan, Groningen, The Netherlands

    P. Tepper, D. Dijkstra & A. S. Horn

Authors
  1. P. M. Beart
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  2. C. J. Cook
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  3. M. Cincotta
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  4. D. J. de Vries
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  5. P. Tepper
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  6. D. Dijkstra
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  7. A. S. Horn
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Beart, P.M., Cook, C.J., Cincotta, M. et al. Radioreceptor binding reveals the potencies of N,N-disubstituted 2-aminotetralins as D2 dopamine agonists. Naunyn-Schmiedeberg's Arch Pharmacol 336, 487–493 (1987). https://doi.org/10.1007/BF00169304

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  • DOI: https://doi.org/10.1007/BF00169304

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