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1 K+‐stimulated release of (3H)‐5‐hydroxytryptamine ((3H)‐5‐HT) from rat frontal cortex slices was decreased by the 5‐HT receptor agonists 5‐methoxy‐n1N‐dimethyltryptamine and 5‐methoxy‐3(1,2,3,6,‐tetrahydro‐4‐pyrindinyl)‐1H‐indole (RU‐24969) (1 × 10−5 M). 2 RU‐24969 (10 mg kg−1, i.p.) decreased extracellular 5‐HT and its metabolite 5‐hydroxyindoleacetic acid measured in vivo by use of intracerebral dialysis combined with high performance liquid chromatography and electrochemical detection. 3 The decrease in extracellular 5‐hydroxyindoleacetic acid in vivo after RU‐24969 (10 mg kg−1, i.p.) was also observed by in vivo voltammetry. 4 The non‐selective 5‐HT antagonist metergoline prevented the RU‐24969‐induced decrease in 5‐HT release and metabolism in vivo while the 5‐HT2 receptor antagonist R‐55669 (ritanserin) did not. 6 The results support the view that RU‐24969 stimulates a 5‐HT1 receptor that is involved in the autoregulation of 5‐HT release and metabolism.
British Journal of Pharmacology – Wiley
Published: Sep 1, 1985
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