Abstract
Extensive characterization of both agonist and antagonist interactions with mammalian D-2 dopamine receptors have been carried out using radioligand binding techniques coupled more recently with computer-assisted data analyses (for review see Creese et al. 1983). However, except for a preliminary study of some novel dopaminergic agonists (Sibley et al., 1982a) no such detailed analyses have been reported describing the interaction of dopaminergic agonists with the D-1 dopamine receptor labeled with [3H]antagonist ligands. Earlier studies indicated that D-1 dopamine receptors in calf and rat striatum can be labeled by the thioxanthene antagonists [3H]flupentixol and [3H]piflutixol (for example Hyttel, 1980). The regional distribution in brain of dopamine-stimulated adenylate cyclase activity and specific, high-affinity [3H]flupentixol binding are similar, and dopaminergic antagonists block both activities with a highly correlated rank-order of potency. Unfortunately [3H]flupentixol is not selective and labels D-2 as well as D-1 dopamine receptors in striatum (Cross and Owen, 1980; Hyttel, 1981; Sibley et al., 1982).
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Creese, I., Leff, S.E. (1986). Regulation of Agonist Interactions with Brain D-1 Dopamine Receptors. In: Woodruff, G.N., Poat, J.A., Roberts, P.J. (eds) Dopaminergic Systems and their Regulation. Satellite Symposia of the IUPHAR 9th International Congress of Pharmacology. Palgrave Macmillan, London. https://doi.org/10.1007/978-1-349-07431-0_6
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DOI: https://doi.org/10.1007/978-1-349-07431-0_6
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