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The peripheral and central anticholinergic properties of benzetimide (R 4929) and other atropine-like drugs as measured in a new anti-pilocarpine test in rats

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Summary

The peripheral and central anticholinergic properties of benzetimide (R 4929) and a series of 22 other atropine-like drugs are measured in a new anti-pilocarpine test in rats. The method, in which a variety of central and peripheral anticholinergic effects can be measured almost simultaneously in the same animal, is described in detail. The results indicate that benzetimide and the chemically related compounds meletimide (R 5183) and cinperene (R 5046) are the only drugs that can block pilocarpine-induced lacrimation or salivation at submydriatic dose levels. Furthermore the relative central anticholinergic potency of these three drugs is quite high and comparable to that of benztropine and the other anticholinergics that are clinically used as antiparkinson-agents.

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  1. Research Laboratoria, Janssen Pharmaceutica, Beerse, Belgium

    Paul A. J. Janssen & Carlos J. E. Niemegeers

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  1. Paul A. J. Janssen
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  2. Carlos J. E. Niemegeers
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Janssen, P.A.J., Niemegeers, C.J.E. The peripheral and central anticholinergic properties of benzetimide (R 4929) and other atropine-like drugs as measured in a new anti-pilocarpine test in rats. Psychopharmacologia 11, 231–254 (1967). https://doi.org/10.1007/BF00405230

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