Neuropharmacology of the anxiolytic
drug opipramol, a sigma site ligand

by
Muller WE, Siebert B, Holoubek G, Gentsch C.
Department of Pharmacology,
Biocenter University Frankfurt,
Marie-Curie-Strasse 9,
D-60439 Frankfurt, Germany.
pharmacolnat@em.uni-frankfurt.de
Pharmacopsychiatry. 2004 Nov;37 Suppl 3:S189-97.


ABSTRACT

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 D (2)-antagonistic and 5-HT2-antagonistic properties cannot be totally be excluded.
Anxiety
Valerian
Gepirone
Buspirone
Zopliclone
Adinazolam
Beta-blockers
Benzodiazepines
Sigma receptors
Future anxiolytics
Opipramol (Insidon)
Low-dose alprazolam
Alprazolam : structure
Alprazolam v tandospirone
Anxiolytics/antidepressants
Alprazolam and panic disorder
Alprazolam-induced hypomania
Alprazolam : discriminative stimulus properties


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