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Pharmacopsychiatry 2004; 37: 189-197
DOI: 10.1055/s-2004-832677
Original Paper
© Georg Thieme Verlag KG Stuttgart · New York

Neuropharmacology of the Anxiolytic Drug Opripramol, a Sigma Site Ligand

W. E. Müller1 , B. Siebert1 , G. Holoubek1 , C. Gentsch2
  • 1Department of Pharmacology, Biocenter University Frankfurt, Frankfurt (Germany)
  • 2Novartis Institutes for Biomedical Research, Neuroscience Disease Area, Basel (Switzerland)
Further Information

Publication History

Publication Date:
17 November 2004 (online)

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Although opipramol is structurally related to imipramine, it does not represent a tricyclic antidepressant drug as it does not inhibit the neuronal uptake of norepinephrine and/or serotonin. Unlike imipramine it is a rather potent sigma ligand with modest subclass selectivity which is similar in vitro as well as ex vivo. Opipramol is active in several behavioural paradigms indicative of anxiolytic properties at doses (1 - 10 mg/kg), which are also needed to occupy sigma binding sites. Somewhat higher doses (10 - 20 mg/kg) are needed for ”antidepressant like” effects. The data allow the conclusion that interaction with sigma sites is involved in the anxiolytic and antidepressant effects of opipramol albeit a contribution of its weaker D2-antagonistic and 5-HT2-antagonistic properties cannot be totally be excluded.

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Prof. Dr. Walter E. Müller

Department of Pharmacology

Biocenter University Frankfurt

Marie-Curie-Str. 9

D-60439 Frankfurt

Phone: #49 69 798 29373

Fax: #49 69 798 29374

Email: pharmacolnat@em.uni-frankfurt.de