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Structure-Activity Relationships of the Butyrophenones and Diphenylbutylpiperidines

  • Chapter
Handbook of Psychopharmacology

Abstract

Shortly after the synthesis (Charpentier, 1950) and pharmacological evaluation of chlorpromazine (Courvoisier et al., 1952), this phenothiazine derivative was recognized to be a most useful antipsychotic agent in the clinic (Delay et al., 1952). The discovery of chlorpromazine, together with the rediscovery of the antipsychotic action of reserpine (Bein, 1953; Kline, 1954), triggered an enormous research effort in many laboratories throughout the world. These two structurally very different types of neuroleptics served as leads for the preparation and subsequent investigation of a tremendous amount of synthetic derivatives. Many of them showed similar pharmacological profiles, but few of them were superior to the original leads. However, it was not until the discovery of the butyrophenones by Janssen et al. (1959a) that a structurally different, although pharmacologically and clinically similar, type of antipsychotic agent was found.

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  1. Research Laboratories, Janssen Pharmaceutica, Beerse, Belgium

    Paul A. J. Janssen & Willem F. M. Van Bever

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  1. Paul A. J. Janssen
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  1. Department of Pharmacology, University of Cambridge, USA

    Leslie L. Iversen

  2. Department of Psychology, University of Cambridge, USA

    Susan D. Iversen

  3. Departments of Pharmacology and Psychiatry, The Johns Hopkins University School of Medicine, USA

    Solomon H. Snyder

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Janssen, P.A.J., Van Bever, W.F.M. (1978). Structure-Activity Relationships of the Butyrophenones and Diphenylbutylpiperidines. In: Iversen, L.L., Iversen, S.D., Snyder, S.H. (eds) Handbook of Psychopharmacology. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-4042-3_1

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