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Relation between the action of dopamine and apomorphine and their O-methylated derivatives upon the CNS

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Summary

The syndrome of gnaw-compulsion was studied in rats providing evidence for a structure-effect relationship between the alcaloid apomorphine and the normal metabolite in the brain, dopamine.

The following tentative conclusions could be drawn from the available data:

  1. 1.

    The phenylethylamine-configuration with an OH-group at the para-position or at both the para- and meta-positions of the phenolring is essential for provoking a gnaw-compulsion syndrome;

  2. 2.

    Replacement of the OH-group at the para-position or at both the para- and meta-position by an OCH3-group antagonizes this effect and induces a hypokinetic state;

  3. 3.

    Occupation of the meta-position by an OH- or OCH3-group in the absence of similar groups at the para-position invariably causes a hyperkinesia.

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Ernst, A.M. Relation between the action of dopamine and apomorphine and their O-methylated derivatives upon the CNS. Psychopharmacologia 7, 391–399 (1965). https://doi.org/10.1007/BF00402361

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