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Quantitative autoradiographic distribution and pharmacological characterization of (3H)buspirone binding to sections from rat, bovine and marmoset brain

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Summary

(3H)Buspirone binds with high affinity (KD =11 nM) to sections from rat striatum. Spiroperidol, chlorpromazine, (+)-butaclamol and apomorphine are the most potent inhibitors of (3H)buspirone binding. Ketanserin, SCH 23390, serotonin and phentolamine are clearly less active. The regional distribution of (3H)buspirone binding in rat and marmoset brain is characterized by high silver grain densities in the olfactory tubercle, nucleus accumbens and striatum. In the hypophysis, the pars intermedia is strongly labeled. Within the hippocampal formation, slightly higher binding site densities are found in the dentate gyrus. The distribution pattern of binding sites in the dentate gyrus varies according to the species investigated. The data presented in this study permit the conclusion that (3H)buspirone binds with high affinity to dopamine2 receptors but do not exclude additional binding to other types of receptors, e.g. 5-HT1 receptors. The interaction of buspirone with dopamine2 receptors may be mainly responsible for its pharmacological profile.

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References

  • Bianchi G, Garattini S (1988) Blockade of α2-adrenoceptors by 1-(2-pyrimidinyl)piperazine (PmP) in vivo and its relation to the activity of buspirone. Eur J Pharmacol 147: 343–350

    PubMed  Google Scholar 

  • Bouthenet ML, Martres MP, Sales N, Schwartz JC (1987) A detailed mapping of dopamine D-2 receptors in rat central nervous system by autoradiography with125I-Iodosulpiride. Neuroscience 20: 117–155

    PubMed  Google Scholar 

  • Brüning G, Kaulen P, Baumgarten HG (1987) Quantitative autoradiographic localization of α2-antagonist binding sites in rat brain using (3H)idazoxan. Neurosci Lett 83: 333–337

    PubMed  Google Scholar 

  • Charuchinda C, Supavilai P, Karobath M, Palacios JM (1987) Dopamine D2 receptors in the rat brain: autoradiographic visualization using a high-affinity selective agonist ligand. J Neurosci 7: 1352–1360

    PubMed  Google Scholar 

  • Desmukh PP, Yamamura HI, Woods L, Nelson DI (1983) Computer-assisted autoradiographic localization of subtypes of serotonin receptors in rat brain. Brain Res 288: 338–343

    PubMed  Google Scholar 

  • Dompert WU, Glaser T, Traber J (1985)3H-TVX Q 7821: identification of 5-HT1 binding sites as target for a novel putative anxiolytic. Naunyn Schmiedebergs Arch Pharmacol 328: 467–470

    PubMed  Google Scholar 

  • Garattini S, Caccia A, Mennini T (1982) Notes on buspirone's mechanisms of action. J Clin Psychiat 43: 19–22

    Google Scholar 

  • Gehlert DR, Wamsley JK (1985) Dopamine receptors in the rat brain: quantitative autoradiographic localization using (3H)sulpiride. Neurochem Int 7: 717–723

    Google Scholar 

  • Glaser T, Traber J (1983) Buspirone: action on serotonin receptors in calf hippocampus. Eur J Pharmacol 88: 137–138

    PubMed  Google Scholar 

  • Glaser T, Rath M, Traber J, Zilles K, Schleicher A (1985) Autoradiographic identification and topographical analysis of high affinity serotonin receptor subtypes as a target for the novel putative anxiolytic TVX Q 7821. Brain Res 385: 129–136

    Google Scholar 

  • Goldberg ME, Salama AJ, Patel JB, Malick JB (1983) Novel non-benzodiazepine axiolytics. Neuropharmacology 22: 1499–1504

    PubMed  Google Scholar 

  • Gozlan H, El Mestikawy S, Pichat L, Glowinski J, Hamon M (1983) Identification of presynaptic serotonin autoreceptors using a new ligand:3H-PAT. Nature 305: 140–142

    PubMed  Google Scholar 

  • Gozlan H, Pouchant M, Daval G, Verge D, Menard F, Vanhove A, Beaucourt JG, Hamon M (1988)125I-Bolton-Hunter-8-Methoxy-2(N-propyl-N-propylamino)tetralin as a new selective radioligand of 5-HT1A sites in the rat brain. In vitro binding and autoradiographic studies. J Pharmacol Exp Ther 244: 751–759

    PubMed  Google Scholar 

  • Kaulen P, Brüning G, Schneider U, Baumgarten HG (1985) Autoradiographic distribution of (3H)buspirone binding sites in rat brain. Neurosci Lett 53: 191–195

    PubMed  Google Scholar 

  • Kaulen P, Brüning G, Rommelspacher H, Baumgarten HG (1986) Characterization and quantitative autoradiography of (3H)buspirone binding sites in rat brain. Neurosci Lett 53: 191–195

    Google Scholar 

  • Köhler C (1984) The distribution of serotonin binding sites in the hippocampal region of the rat brain. An autoradiographic study. Neuroscience 13: 667–680

    PubMed  Google Scholar 

  • Lightman SL, Ninkovic M, Hunt SP (1982) Localization of (3H)spiperone binding sites in the intermediate lobe of the rat pituitary gland. Neurosci Lett 32: 99–102

    PubMed  Google Scholar 

  • McMillan BA, Scott SM, Williams HL, Sanghera MK (1987) Effects of gepirone, an arylpiperazine anxiolytic drug, on aggressive behavior and brain monoaminergic neurotransmission. Naunyn Schmiedebergs Arch Pharmacol 335: 454–464

    PubMed  Google Scholar 

  • McPherson GA (1985) Analysis of radioligand binding experiments: a collection of computer programs for the IBM PC. J Pharmacol Methods 14: 213–222

    PubMed  Google Scholar 

  • Meert TF, Colpaert FC (1986) The shock-probe conflict procedure. A new assay responsive to benzodiazepines, barbiturates and related compounds. Psychopharmacology 88: 455–450

    Google Scholar 

  • Meibach RC, Beck SG, Maayani S, Green JP (1982) Regional differences in binding of (3H)5-HT in calf hippocampal slices revealed by radioautography and rapid filtration studies. Brain Res 307: 69–75

    Google Scholar 

  • Meltzer HY, Fleming R (1982) Effect of buspirone on prolactin and growth hormone secretion in laboratory rodents and man. J Clin Psychiat 43: 76–79

    Google Scholar 

  • Pellow S, File SE (1986) Anxiolytic and anxiogenic drug effects on exploratory activity in an elevated plus-maze: a novel test of anxiety in the rat. Pharmacol Biochem Behav 24: 525–529

    PubMed  Google Scholar 

  • Peroutka SJ (1985) Selective interaction of novel anxiolytics with 5-hydroxytryptamine1A receptors. Biol Psychiat 20: 971–979

    PubMed  Google Scholar 

  • Riblet LA, Eison AS, Eison MS, Taylor DP, Temple DL, Van der Maelen CP (1984) Neuropharmacology of buspirone. Psychopathology 17 [Suppl 3]: 69–78

    PubMed  Google Scholar 

  • Riblet LA, Taylor DP, Eison MS, Stanton HC (1982) Pharmacology and neurochemistry of buspirone. J Clin Psychiat 43: 11–16

    Google Scholar 

  • Rothman RB, Herkenham M, Pert CB, Liang TL, Cascieri MA (1984) Visualization of rat brain receptors for the neuropeptide, substance P. Brain Res 309: 47–54

    PubMed  Google Scholar 

  • Skolnick P, Weissmann BA, Youdim MBH (1985) Monoaminergic involvement in the pharmacological actions of buspirone. Br J Pharmacol 86: 637–644

    PubMed  Google Scholar 

  • Stanley M, Russo A, Gershon S (1979) The effect of MJ 9022-1 on striatal DOPAC and apomorphine-induced stereotyped behavior in the rat. Res Commun Psychol Psychiat Behav 4: 127–134

    Google Scholar 

  • Stanton HC, Taylor DP, Riblet LA (1981) Buspirone—an anxioselective drug with dopaminergic action. In: Chronister RB, DeFrance JF (eds) The neurobiology of the nucleus accumbens. Haer Institute Brunswick, pp 316–321

  • Theodorou A, Crockett M, Jenner P, Marsden CD (1979) Specific binding of (3H)-sulpiride to rat striatal preparations. J Pharm Pharmacol 31: 424–426

    PubMed  Google Scholar 

  • Wood PL, Nair NPV, Lal S, Etienne P (1983) Buspirone: a potential atypical neuroleptic. Life Sci 33: 269–273

    PubMed  Google Scholar 

  • Zahniser NR, Molinoff PB (1978) Effect of guanine nucleotides on striatal dopamine receptors. Nature 272: 453–455

    Google Scholar 

  • Zilles K, Schleicher A, Rath M, Glaser T, Traber J (1986) Quantitative autoradiography of transmitter binding sites with an image analyzer. J Neurosci Methods 18: 207–220

    PubMed  Google Scholar 

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Brüning, G., Kaulen, P., Schneider, U. et al. Quantitative autoradiographic distribution and pharmacological characterization of (3H)buspirone binding to sections from rat, bovine and marmoset brain. J. Neural Transmission 78, 131–144 (1989). https://doi.org/10.1007/BF01252499

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  • DOI: https://doi.org/10.1007/BF01252499

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