Abstract
CONSIDERABLE evidence suggests that antipsychotic drugs block dopamine receptors at postsynaptic sites in the central nervous system1,2. Receptor sites for neurotransmitter substances, such as acetylcholine3–5 and glycine6, have been studied by measurements of the direct binding of radiolabelled compounds that have high affinity for such sites and cause receptor blockade. In a similar study of biogenic amine receptor sites, I have measured the binding and displacement of the potent phenothiazine antipsychotic drug, fluphenazine, to preparations of brain tissue in vitro. I have found that fluphenazine binds to all regions of the rat brain, and that the potency of antipsychotic drugs in displacing fluphenazine correlates well with their clinical efficacy. Dopamine does displace fluphenazine from binding sites, but this is a nonspecific effect shared by other biogenic amines.
This is a preview of subscription content, access via your institution
Access options
Subscribe to this journal
Receive 51 print issues and online access
$199.00 per year
only $3.90 per issue
Buy this article
- Purchase on Springer Link
- Instant access to full article PDF
Prices may be subject to local taxes which are calculated during checkout
Similar content being viewed by others
References
Kebabian, J. W., Petzold, G. L., and Greengard, P., Proc. natn. Acad. Sci. U.S.A., 69, 2145–2149 (1972).
Miller, R. J., and Iversen, L. L., Trans. biochem. Soc., 2, 256–259 (1974).
De Robertis, E., Science, 171, 963–971 (1971).
Farrow, J. T., and O'Brien, R. D., Molec. Pharmac., 9, 33–40 (1973).
Yamamura, H. I., and Snyder, S. H., Proc. natn. Acad. Sci. U.S.A., 71, 1725–1729 (1974).
Young, A. B., and Snyder, S. H., Proc. natn. Acad. Sci. U.S.A., 70, 2832–2836 (1973).
Hornykiewicz, O., Pharmac. Rev., 18, 925–964 (1966).
Rang, H. P., Br. J. Pharmac., 48, 475–495 (1973).
Lowry, O. H., Rosebrough, N. J., Fair, A. L., and Randall, R. J., J. biol Chem., 193, 265–275 (1951).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
TAYLOR, K. Displacement of bound 14C-fluphenazine by biogenic amines and antipsychotic drugs in homogenates of brain tissue. Nature 252, 238–241 (1974). https://doi.org/10.1038/252238a0
Received:
Revised:
Issue Date:
DOI: https://doi.org/10.1038/252238a0
Comments
By submitting a comment you agree to abide by our Terms and Community Guidelines. If you find something abusive or that does not comply with our terms or guidelines please flag it as inappropriate.