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In rat brain cortex slices preincubated with [³H]5-HT, the potencies of 17 5-HT receptor agonists to inhibit the electrically evoked³H overflow and the affinities of 13 antagonists (including several β-adrenoceptor blocking agents) to antagonize competitively the inhibitory effect of unlabelled 5-HT on evoked³H overflow were determined.

The affinities of the compounds for 5-HT_1B and 5-HT₂ binding sites in rat brain cortex membranes (labelled by [¹²⁵I]cyanopindolol = [¹²⁵I]-CYP in the presence of 30 μmol/l isoprenaline and [³H]ketanserin, respectively), for 5-HT_1A binding sites in pig and rat brain cortex membranes (labelled by [³H]8-hydroxy-2-(di-n-propylamino)tetralin = [³H]8-OH-DPAT) and for 5-HT_1C binding sites in pig choroid plexus membranes (labelled by [³H …