Effects of chronic oral administration of the antidepressants, desmethylimipramine and zimelidine on rat cortical GABAB binding sites: a comparison with 5‐HT2 binding site changes

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Abstract
The effects of chronic oral administration of desmethylimipramine (DMI) or zimelidine (1.25 and 5 mg kg−1 twice daily for 21 days) were studied on rat whole cortical γ‐aminobutyric acidB (GABAB) binding sites. No changes in receptor affinity or number were found with either drug. A subsequent study of GABAB binding sites using higher doses of these drugs (5 and 10 mg kg−1) and rat frontal cortex was also without effect, when investigated 24 h after termination of drug administration or 72 h after DMI administration (5 mg kg−1). The number of frontal cortical 5‐hydroxytryptamine2 (5‐HT2) binding sites was significantly and dose‐dependently decreased after both drugs, whereas the number of hippocampal 5‐HT2 binding sites was not significantly altered after either drug. As the number of frontal cortical GABAB binding sites was unaltered whereas the number of 5‐HT2 binding sites was significantly decreased under identical study conditions, it may be concluded that the effects of antidepressant administration upon GABAB binding sites is a less consistent observation than their effects on 5‐HT2 binding sites.

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