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Serotonergic agonists behave as partial agonists at the dopamine D2 receptor

descriptionPublicationkeyboard_double_arrow_right Article 01 Feb 1999Publisher:Ovid Technologies (Wolters Kluwer Health)Journal:NeuroReport, volume 10, pages 493-495 (issn: 0959-4965,

Authors: Sergi Ferré; Kjell Fuxe; Anton Terasmaa; Ago Rinken; Christer Owman;

doi: 10.1097/00001756-199902250-00009

pmid: 10208577

Serotonergic agonists behave as partial agonists at the dopamine D2 receptor

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Abstract

RAT dopamine D2short receptors expressed in CHO cells were characterized by activation of [35S]GTPgammaS binding. There were no significant differences between the maximal effects seen in activation of [35S]GTPgammaS binding caused by dopaminergic agonists, but the effects of 5-HT, 8OH-DPAT and 5-methoxytryptamine amounted to 47 +/- 7%, 43 +/- 5% and 70 +/- 7% of the dopamine effect, respectively. The dopaminergic antagonist (+)butaclamol inhibited activations of both types of ligands with equal potency (pA2 = 8.9 +/- 0.1), indicating that only one type of receptor is involved. In competition with [3H]raclopride binding, dopaminergic agonists showed 53 +/- 2% of the binding sites in the GTP-dependent high-affinity state, whereas 5-HT showed only 20 +/- 3%. Taken together, the results indicate that serotonergic agonists behave as typical partial agonists for D2 receptors with potential antiparkinsonian activity.

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Keywords

8-Hydroxy-2-(di-n-propylamino)tetralin, Serotonin, Dose-Response Relationship, Drug, Receptors, Dopamine D2, Cell Membrane, CHO Cells, Serotonin Receptor Agonists, 5-Methoxytryptamine, Guanosine 5'-O-(3-Thiotriphosphate), Raclopride, Cricetinae, Dopamine Agonists, Salicylamides, Animals, Dopamine Antagonists, Butaclamol

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