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It has been hypothesized that 5‐HT1A autoreceptor antagonists may enhance the therapeutic efficacy of SSRIs and other antidepressants. Although early clinical trials with the β‐adrenoceptor/5‐HT1 ligand, pindolol, were promising, the results of recent more extensive trials have been contradictory. Here we investigated the actions of pindolol at the 5‐HT1A autoreceptor by measuring its effect on 5‐HT neuronal activity and release in the anaesthetized rat. Pindolol inhibited the electrical activity of 5‐HT neurones in the dorsal raphe nucleus (DRN). This effect was observed in the majority of neurones tested (10/16), was dose‐related (0.2–1.0 mg kg−1, i.v.), and was reversed by the 5‐HT1A receptor antagonist, WAY 100635 (0.1 mg kg−1, i.v.), in 6/7 cases tested. Pindolol also inhibited 5‐HT neuronal activity when applied microiontophoretically into the DRN in 9/10 neurones tested. This effect of pindolol was current‐dependent and blocked by co‐application of WAY 100635 (3/3 neurones tested). In microdialysis experiments, pindolol caused a dose‐related (0.8 and 4 mg kg−1, i.v.) fall in 5‐HT levels in dialysates from the frontal cortex (under conditions where the perfusion medium contained 1 μM citalopram). In rats pretreated with WAY 100635 (0.1 mg kg−1, i.v.), pindolol (4 mg kg−1, i.v.) did not decrease, but rather increased 5‐HT levels. We conclude that, under the experimental conditions used in this study, pindolol displays agonist effects at the 5‐HT1A autoreceptor. These data are relevant to previous and ongoing clinical trials of pindolol in depression which are based on the rationale that the drug is an effective 5‐HT1A autoreceptor antagonist.
British Journal of Pharmacology – Wiley
Published: May 1, 1998
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