Abstract
THE pharmacological activity of (±) benzetimide (Fig. 1) ((±)-1-benzyl-4-(2,6-dioxo-3-phenyl-3-piperidyl)-piperidine HCl), a potent and persistent anticholinergic agent, acting in both the peripheral and the central nervous system, is due entirely to the (+)-isomer dexbenzetimide1. The drug is used to abolish Parkinson symptoms sometimes evoked in psychiatric patients being treated with neuroleptic drugs2. The anticholinergic properties are due to the unaltered dexbenzetimide and not to its metabolites3. As dexbenzetimide is specifically taken up and retained by small nerve endings of the caudate nucleus of the rat3, it is tempting to assume that the binding sites are at or near an acetylcholine receptor.
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References
Janssen, P. A. J., Niemegeers, C. J. E., Schellekens, K. H. L., Demoen, P., Lenaerts, F. M., Van Nueten, J. M., van Wijngaarden, I., and Brugmans, J., Arzneimittel-Forsch. (in the press).
De Smedt, R., Rodrigus, E., Debandt, R., and Brugmans, J., J. Clin. Pharmacol., 10, 207 (1970).
van Wijngaarden, I., Life Sci., 1, 9, 489 (1970).
van Wijngaarden, I., thesis, Univ. Leyden (1970).
van Wijngaarden, I., Soudijn, W., and Van der Eycken, C., Life Sci., 9, 1289 (1970).
Archer, S., Lands, A. M., and Lewis, T. R., J. Med. Pharmacol. Chem., 5, 423 (1962).
Chothia, C., and Pauling, P., Nature, 226, 541 (1970).
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SPEK, A., PEERDEMAN, A., VAN WIJNGAARDEN, I. et al. The Absolute Configuration and Crystal Structure of the Anticholinergic Drug Dexbenzetimide. Nature 232, 575–576 (1971). https://doi.org/10.1038/232575a0
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DOI: https://doi.org/10.1038/232575a0
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