Nature Publishing Group, publisher of Nature, and other science journals and reference works
my account e-alerts subscribe register
Wednesday 23 August 2017
Journal Home
Current Issue
Download PDF
Export citation
Export references
Send to a friend
More articles like this

Letters to Nature
Nature 261, 717 - 719 (24 June 1976); doi:10.1038/261717a0

Antipsychotic drug doses and neuroleptic/dopamine receptors


Department of Pharmacology, University of Toronto, Toronto, Canada M5S LA8

ANTIPSYCHOTIC drugs, or neuroleptics, are thought to act by blocking dopamine receptors in the nervous system1–4. Recent direct evidence, based on stereospecific binding assays, supports this hypothesis of antipsychotic drug action5–9. As only a few antipsychotic drugs had been tested for their effects on the binding of haloperidol5–8, the question remained whether all antipsychotic drugs, regardless of chemical structure, would block the stereospecific binding of haloperidol. We report here that all clinically effective antipsychotic drugs (tested so far) block the stereo-specific binding of 3H-haloperidol at concentrations which correlate directly with the clinical potencies.



1. Van Rossum, J. M., Arch. int. Pharmacodyn., 160, 492–494 (1966).
2. Iversen, L. L., Science, 188, 1084–1089 (1975).
3. Horn, A. S., Post, M. L., and Kennard, O., J. Pharm. Pharmac., 27, 553–563 (1975).
4. Matthysse, S., Fedn Proc., 32, 200–204 (1973).
5. Seeman, P., Wong, M., and Lee, T., Fedn Proc., 33, 246 (1974).
6. Seeman, P., Wong, M., and Tedesco, J., Proc. Neurosci. Soc., 5, 405 (1975).
7. Seeman, P., Chau-Wong, M., Tedesco, J., and Wong, K., Proc. natn. Acad. Sci. U.S.A., 72, 4376–4380 (1975).
8. Creese, I., Burt, D. R., and Snyder, S. H., Life Sci., 17, 993–1002 (1975).
9. Burt, D. R., Enna, S., Creese, I., and Snyder, S. H., Proc. natn. Acad. Sci. U.S.A., 72, 4655–4659 (1975).
10. Seeman, P., Pharmac. Rev., 24, 583–655 (1972).
11. Seeman, P., Staiman, A., and Chau-Wong, M., J. Pharmac. exp. Ther., 190, 123–130 (1974).
12. Seeman, P., and Lee, T., Science, 188, 1217–1219 (1975).
13. Seeman, P., in Antipsychotic Drugs, Pharmacodynamics and Pharmacokinetics (edit. by Sedvall, G.) (Pergamon, Oxford, in the press).
14. Forsman, A., Ma ringrtensson, E., Nyberg, G., and Ohman, R., Naunyn–Schmiedeberg's Arch. Pharmac., 286, 113–124 (1974).
15. Sakalis, G., Curry, S. H., Mould, G. P., and Lader, M. H., Clin. Pharmac. Ther., 13, 931–946 (1972).
16. Cooper, S. F., Albert, J.-M., Hillel, J., and Caille, G., Curr. Ther. Res., 15, 73–77 (1973).
17. Pecknold, J. C., Ban, T. A., Lehmann, H. E., and Climan, M., Int. J. clin. Pharmac., 11, 299–303 (1975).
18. Simpson, G. M., and Varga, V., Curr. Ther. Res., 16, 477–482 (1974).

© 1976 Nature Publishing Group
Privacy Policy