Abstract

5-HT 3 receptors have been localized in the rat brain using the selective antagonist ligand [ 3H]LY278584. The binding of this ligand to slide mounted tissue sections was characterized by a K d value of 1.5 nM and a B max value of 110 fmol/mg tissue dry weight. The specific binding was displaced by 5-HT or a number of 5-HT 3 antagonist compounds. High densities of 5-HT 3 receptors were detected in the nucleus of the solitary tract, dorsal motor nucleus of the vagus and area postrema. Moderate levels of binding were found in the glomerular layer of the olfactory bulb, substantia gelatinosa of the trigeminal nucleus and spinal cord and various nuclei of the amygdala. Low levels of binding were found in the superficial laminae of the cerebral cortex and relatively evenly distributed in the hippocampus. These results indicate that [ 3H]LY278584 is a useful ligand to study 5-HT 3 receptors by quantitative autoradiography.

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