1 The 5‐HT4 receptor antagonist, GR113808, has been radiolabelled to a high specific activity with tritium. 2 Characterization of specific (3H)‐GR113808 binding in homogenates of guinea‐pig striatum and hippocampus revealed a single site of high affinity (Kd values 0.20 and 0.13 nm respectively). 3 (3H)‐GR113808 binding was reversible and displayed rapid kinetics such that association and dissociation were complete within 3 min. 4 Specific (3H)‐GR113808 binding was potently and stereoselectively inhibited by agonists and antagonists acting at the 5‐HT4 receptor but not by compounds selective for other 5‐HT receptors or other neurotransmitter receptors. 5 Autoradiographic analysis revealed a discrete localization in both guinea‐pig and rat brain with high concentrations of binding in brain areas such as the striatum, substantia nigra and olfactory tubercle. 6 (3H)‐GR113808 binding to homogenates of guinea‐pig striatum meets the criteria for labelling of the 5‐HT4 receptor and, as such, represents the first characterization of this receptor in a radioligand binding assay.
British Journal of Pharmacology – Wiley
Published: Jul 1, 1993
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