Abstract
In 1968 Belleau and associates (Belleau et al., 1968) reported that the peptide coupling agent N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) was a potent and irreversible α-adrenergic receptor antagonist. Subsequent in vitro studies in peripheral tissues by Chang et al. (1970) and Kalsner (1973) revealed that it could also irreversibly inactivate muscarinic cholinergic and serotonergic receptors, respectively. There was relatively little interest in this agent, however, until Hamblin and Creese (1983) demonstrated its ability to irreversibly block central dopamine (DA) receptors as well. In this article we will review the growing number of studies which have successfully utilized this agent to generate important new insights into the function of several CNS receptors, with special emphasis on dopamine (DA) receptors. Pertinent examples from our own studies on DA receptors will be presented, and its application to the determination of the relationship between receptor occupancy and response for agonists at CNS receptors mediating various functional effects will be highlighted.
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Meller, E., Goldstein, M., Friedhoff, A.J., Schweitzer, J.W. (1988). N-Ethoxycarbonyl-2-Ethoxy-1, 2-Dihydroquinoline (EEDQ): A New Tool to Probe CNS Receptor Function. In: Goldstein, M., Fuxe, K., Tabachnick, I. (eds) Central D1 Dopamine Receptors. Advances in Experimental Medicine and Biology, vol 235. Springer, Boston, MA. https://doi.org/10.1007/978-1-4899-2723-1_8
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DOI: https://doi.org/10.1007/978-1-4899-2723-1_8
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