Skip to main content
Log in

[3H]-Domperidone labels only a single population of receptors which convert from high to low affinity for dopamine in rat brain

  • Published:
Naunyn-Schmiedeberg's Archives of Pharmacology Aims and scope Submit manuscript

Summary

Dopamine recognized and competed for a single population of [3H]-domperidone-binding sites in rat striatum and olfactory tubercle when tested in the presence of sodium ions and guanine nucleotide [Gpp(NH)p]. In the absence of Na+ and Gpp(NH)p, however, dopamine recognized two components of [3H]-domperidone binding. Thus, [3H]-domperidone labelled only a single population of dopamine receptors (type D2) which fully converted from high to low affinity for dopamine. These results agree with those found previously using [3H]-spiperone and [3H]-YM-09151-2.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  • Baudry M, Martres MP, Schwartz JC (1979)3H-Domperidone: A selective ligand for dopamine receptors. Naunyn-Schmiedeberg's Arch Pharmacol 308:231–237

    Google Scholar 

  • Fleming WW, Westfall DP, De la Lande IS, Jellet LB (1972) Lognormal distribution of equieffective doses of norepinephrine and acetylcholine in several tissues. J Pharmacol Exp Ther 181:339–345

    Google Scholar 

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

    Google Scholar 

  • Grigoriadis D, Seeman P (1984) The dopamine/neuroleptic receptor. Can J Neurol Sci 11:108–113

    Google Scholar 

  • Grigoriadis D, Seeman P (1985) Complete conversion of brain D2 dopamine receptors from the high- to the low-affinity state for dopamine agonists, using sodium ions and guanine nucleotide. J Neurochem 44:1929–1935

    Google Scholar 

  • Hamblin MW, Leff SE, Creese I (1984) 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(6):877–887

    Google Scholar 

  • Huff RM, Molinoff PB (1982) Quantitative determination of dopamine receptor subtypes not linked to activation of adenylate cyclase in rat striatum. Proc Nat Acad Sci (USA) 79:7561–7565

    Google Scholar 

  • Jenner P, Elliott PNC, Clow A, Reavill C, Marsden CD (1978) A comparison of in vitro and in vivo dopamine receptor antagonism produced by substituted benzamide drugs. J Pharm Pharmacol 30:46–48

    Google Scholar 

  • Lazareno S (1983) Effects of GTP on3H-domperidone binding and its displacement by dopamine in rat striatal homogenates. J Recept Res 3(1&2):163–175

    Google Scholar 

  • Leysen JE, Niemegeers CJE, Van Neuten JM, Laduron PM (1978) Spiperone: A ligand of choice for neuroleptic receptors. 1. Kinetics and characteristics of in vitro binding. Biochem Pharmacol 27:307–316

    Google Scholar 

  • Martres MP, Baudry M, Schwartz JC (1978) Characterization of3H-domperidone binding on striatal dopamine receptors. Life Sci 23:1781–1784

    Google Scholar 

  • Munson PJ, Rodbard D (1980) A versatile computerized approach for characterization of ligand-binding systems. Anal Biochem 107:220–239

    Google Scholar 

  • Niznik HB, Grigoriadis D, Pri-Bar I, Buchman O, Seeman P (1985) Dopamine D2 receptors selectively labeled by a benzamide neuroleptic: [3H]-YM-09151-2. Naunyn-Schmiedeberg's Arch Pharmacol 329:333–343

    Google Scholar 

  • Sokoloff P, Martres MP, Delandre M, Redouane K, Schwartz JC (1984)3H-Domperidone binding sites differ in rat striatum and pituitary. Naunyn-Schmiedeberg's Arch Pharmacol 327:221–227

    Google Scholar 

  • Sokoloff P, Protais P (1984b) In: Woodruff GN, Creese I, Gessa GL, Hornykiewicz O, Poat JA, Roberts PJ (eds) Dopaminergic systems and their regulation. Macmillan Press, London (in press)

    Google Scholar 

  • Sokoloff P, Redouane K, Brann M, Martres MP, Schwartz JC (1985)3H-(−)DO 710 discriminates guanine nucleotide sensitive and insensitive dopamine binding sites. Naunyn-Schmiedeberg's Arch Pharmacol 329:236–243

    Google Scholar 

  • Wreggett KA, Seeman P (1984) Agonist high-and low-affinity states of the D2 dopamine receptor in calf brain: Partial conversion by guanine nucleotide. Mol Pharm 25:10–17

    Google Scholar 

  • Zahniser NR, Molinoff PB (1978) Effect of guanine nucleotides on striatal dopamine receptors. Nature 275:453–455

    Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Cite this article

Grigoriadis, D., Seeman, P. [3H]-Domperidone labels only a single population of receptors which convert from high to low affinity for dopamine in rat brain. Naunyn-Schmiedeberg's Arch. Pharmacol. 332, 21–25 (1986). https://doi.org/10.1007/BF00633192

Download citation

  • Received:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF00633192

Key words

Navigation