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Dopamine D1 and D2 Receptor Selectivities of Agonists and Antagonists

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Part of the book series: Advances in Experimental Medicine and Biology ((AEMB,volume 235))

Summary

The selectivities of various dopamine agonists and antagonists for dopamine D1 and D2 receptors were obtained by comparing their relative dissociation constants for inhibiting the binding of [3H]SCH 23390 at D1 receptors (calf caudate nucleus) and at D2 receptors (pig anterior pituitary tissue). The most selective agonists were SK&F 38393 (for D1) and (+)-PHNO (for D2), while the most selective antagonists were SCH 23390 (for D1) and raclopride or eticlopride (for D2).

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References

  • Flaim K.E., Gessner G.W., Crooke S.T., Weinstock J. and Heys J.R. (1985) Characterization of agonist binding to D1 receptors in rat striatum using the D1 selective antagonists 3H-SKF R-83566. Fed. Proc. 44, 1832.

    Google Scholar 

  • George S.R., Watanabe M. and Seeman P. Dopamine D2 receptors in the anterior pituitary: A single population without reciprocal agonist/antagonist states. J. Neurochem. 44: 1168–1177 (1985a).

    Article  Google Scholar 

  • George S.R., Watanabe M. and Seeman P. Dopamine D2 receptors in brain and anterior pituitary recognize agonist and antagonist actions of (-)-3-PPP. J. Neural Transm. 64: 13–33 (1985).

    Article  Google Scholar 

  • George S.R., Watanabe ML, Di Paolo T., Falardeau P., Labrie F. and Seeman P. The functional state of the dopamine receptor in the anterior pituitary is in the high-affinity form. Endocrinology 117: 690–697 (1985b).

    Article  Google Scholar 

  • Grigoriadis D. and Seeman P. Complete conversion of brain D2 dopamine receptors from the high-to low-affinity state for dopamine agonists, using sodium ions and guanine nucleotide. J. Neurochem. 44: 1925–1935 (1985).

    Article  Google Scholar 

  • Hamblin M.W., Leff S.E. and Creese I. Interactions of agonists with D-2 dopamine receptors: evidence for a single receptor population existing in multiple agonist affinity-states in rat striatal membranes. Biochem. Pharmacol. 33: 877–887 (1984).

    Article  Google Scholar 

  • Munson P. and Rodbard D. “Ligand”: A versatile computerized approach for characterization of ligand-binding systems. Anal. Biochem. 107: 220–239 (1980).

    Article  Google Scholar 

  • O’Boyle K.M. and Waddington J.L. [3H]SCH 23390 binding to human putamen D-1 dopamine receptors: Stereochemical and structure-affinity relationships among l-Phenyl-1H-3-benzazepine derivatives as a guide to D-1 receptor topography. J. Neurochem. 48: 1039–1042 (1987).

    Article  Google Scholar 

  • Seeman P. The absolute density of neurotransmitter receptors in brain: example for dopamine receptors. J. Pharmacol. Methods 17: 347–360 (1987).

    Article  Google Scholar 

  • Seeman P. and Grigoriadis D. Dopamine receptors in brain and periphery. Neurochem. Int. 10: 1–25 (1987).

    Article  Google Scholar 

  • Seeman P. and Grigoriadis D. Dopamine D2 receptor dissociation constant for spiperone: identical values using 3H-labeled agonist or 3H-labeled antagonist. Biochem. Pharmacol. 34: 4065–4066 (1985).

    Article  Google Scholar 

  • Seeman P., Watanabe M., Grigoriadis D., Tedesco J.L., George S.R., Svensson U., Nilsson J.L.G. and Neumeyer J.L. Dopamine D2 receptor binding sites for agonists: a tetrahedral model. Mol. Pharmacol. 28: 391–399 (1985a).

    Google Scholar 

  • Seeman P., Ulpian C., Grigoriadis D., Pri-Bar I. and Buchman O. Conversion of dopamine D1 receptors from high to low affinity for dopamine. Biochem. Pharmacol. 34: 151–154 (1985b).

    Article  Google Scholar 

  • Seeman P. Brain dopamine receptors. Pharmacol. Rev. 32: 229–313 (1980).

    Google Scholar 

  • Stoof J.C. and J.W. Kebabian. Two dopamine receptors: biochemistry, physiology and pharmacology. Life Sci. 35: 2281–2296 (1984).

    Article  Google Scholar 

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© 1988 Springer Science+Business Media New York

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Seeman, P., Ulpian, C. (1988). Dopamine D1 and D2 Receptor Selectivities of Agonists and Antagonists. 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_5

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  • DOI: https://doi.org/10.1007/978-1-4899-2723-1_5

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4899-2725-5

  • Online ISBN: 978-1-4899-2723-1

  • eBook Packages: Springer Book Archive

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