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Harikumar KG, Chattopadhyay A: Modulation of antagonist binding to serotonin1A receptors from bovine hippocampus by metal ions. Cell Mol Neurobiol. 2001 Oct;21(5):453-64.
1. The serotonin1A (5-HT1A) receptors are members of a superfamily of seven transmembrane domain receptors that couple to G-proteins. They appear to be involved in various behavioral and cognitive functions. Although specific 5-HT1A agonists have been discovered more than a decade back, the development of selective 5-HT1A antagonists has been achieved only recently. 2. We have examined the modulation of the specific antagonist [3H] p-MPPF binding to 5-HT1A receptors from bovine hippocampal membranes by monovalent and divalent metal ions. Our results show that the antagonist binding to 5-HT1A receptors is inhibited by both monovalent and divalent cations in a concentration-dependent manner. This is accompanied by a concomitant reduction in binding affinity. 3. Our results also show that the specific antagonist p-MPPF binds to all available receptors in the bovine hippocampal membrane irrespective of their state of G-protein coupling and other serotonergic ligands such as 5-HT and OH-DPAT effectively compete with the specific antagonist [3H] p-MPPF. 4. These results are relevant to ongoing analyses of the overall modulation of ligand binding in G-protein-coupled seven transmembrane domain receptors. |
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