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Specific modulation of sigma binding sites by the anxiolytic drug opipramol

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Summary.

 The atypical anxiolytic and antidepressive drug opipramol binds with high affinity to σ1 and somewhat lower affinity to σ2 sites. After subchronic treatment, opipramol significantly down-regulated σ2 but not σ1 sites. This effect was not seen for imipramine, citalopram, and reboxetine under similar conditions. On the other hand, only imipramine reduced the number of σ1 sites. It is suggested that effects at σ2 sites are involved in the anxiolytic properties of opipramol.

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Received February 7, 2003; accepted March 24, 2003 Published online July 30, 2003

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Holoubek, G., Müller, W. Specific modulation of sigma binding sites by the anxiolytic drug opipramol. J Neural Transm 110, 1169–1179 (2003). https://doi.org/10.1007/s00702-003-0019-5

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  • DOI: https://doi.org/10.1007/s00702-003-0019-5

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