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3H-spiroperidol binding in human temporal cortex (brodmann areas 41–42) occurs at multiple high affinity states with serotonergic selectivity

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Abstract

3H-Spiroperidol labels multiple high affinity states with serotonergic selectivity in human prefrontal cortex and with dopaminergic selectivity in human caudate and putamen. The characteristics of the binding of this ligand in human temporal cortex have not been previously described. Brodmann areas 41–42 in the temporal cortex are associated with primary auditory sensation and, in epileptics, with auditory hallucinatory experiences. We found that in this region of the human brain, antipsychotic ligands bind at multiple high affinity states, the majority of which exhibit serotonergic, rather than dopaminergic, selectivity. Dose-response data is best resolved by a three-site fit. Results of the co-analysis of dose-response data with saturation data indicates that two of the3H-spiroperidol affinity states may represent the high and low affinity states of the serotonin (5HT)2 receptor, while a third affinity state may represent the 5-HT1A receptor.

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References

  • Altar CA, Kim H, Marshall JF (1985) Computer imaging and analysis of dopamine (D2) and serotonin (S2) binding sites in rat basal ganglia or neocortex labeled by [3H]spiroperidol. J Pharmacol Exp Ther 233:527–538

    Google Scholar 

  • Andorn AC (1986) Do antipsychotic drugs and serotonin down regulate [3H]-spiroperidol binding sites in human cortex? Life Sci 38:1251–1260

    Google Scholar 

  • Andorn AC, Huang EH, Warren AE (1984) Specific [3H]-spiroperidol binding sites in human prefrontal cortex: potential site multiplicity and overall serotonin-like selectivity. Life Sci 34:2461–2466

    Google Scholar 

  • Andorn AC, Carlson MA, Gilkeson RC (1988) Specific [3H]UK 14304 binding in human cortex occurs at multiple high affinity states with alpha2-adrenergic selectivity and differing affinities for GTP. Life Sci 43:1805–1812

    Google Scholar 

  • Arnett CD, Wolf AP, Chyng-Yann S, Fowler JS, MacGregor RR, Christman DR, Smith M (1986) Improved delineation of human dopamine receptors using [18F]-N-methylspiroperidol and PET. J Nucl Med 27:1878–1882

    Google Scholar 

  • Asaad G, Shapiro B (1986) Hallucinations: theoretical and clinical overview. Am J Psychiatry 143:1088–1097

    Google Scholar 

  • Conn PJ, Sanders-Bush E (1987) Central serotonin receptors: effector systems, physiological roles and regulation. Psychopharmacology 92:267–277

    Google Scholar 

  • Forster C, Whalley ET (1981) Spiperone contracts the human basilar arterial strip in vitro: possible interaction with 5-hydroxy-tryptamine receptors? Br J Pharmacol 72:581P-582P

    Google Scholar 

  • Lidov HG, Grzanna R, Molliver ME (1980) The serotonin innervation of the cerebral cortex in the rat — an immunohistochemical analysis. Neuroscience 5:207–227

    Google Scholar 

  • Lowry OH, Rosebrough NJ, Farr AL, Randall RJ (1951) Protein measurement with the Folin phenol reagent. J Biol Chem 193:265–275

    Google Scholar 

  • McPherson GA (1985) Analysis of radioligand binding experiments: a collection of computer programs for the IBM PC. J Pharmacol Methods 14:213–228

    Google Scholar 

  • Mita T, Susumu H, Nishino N, Kuno T, Nakai H, Yamadori T, Mizoi Y, Tanaka C (1986) Decreased serotonin S2 and increased dopamine D2 receptors in chronic schizophrenics. Biol Psychiatry 21:1407–1414

    Google Scholar 

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

    Google Scholar 

  • Pedigo NW, Yamamura HI, Nelson DL (1981) Discrimination of multiple [3H]5-hydroxytryptamine binding sites by the neuroleptic spiperone in rat brain. J Neurochem 36:220–226

    Google Scholar 

  • Penfield W, Jasper H (1954) Epilepsy and the functional anatomy of the human brain. Little Brown and Company, Boston

    Google Scholar 

  • Peroutka SJ (1986) Pharmacological differentiation and characterization of 5-HT1A, 5-HT1B, and 5-HT1C binding sites in rat frontal cortex. J Neurochem 47:529–540

    Google Scholar 

  • Peroutka SJ, Snyder SH (1980) Relationship of neuroleptic drug effects at brain dopamine, serotonin, α-adrenergic, and histamine receptors to clinical potency. Am J Psychiatry 137:1518–1522

    Google Scholar 

  • Titeler M, Lyon RA, Davis KH, Glennon RA (1987) Selectivity of serotonergic drugs for multiple brain serotonin receptors. Role of [3H]-4-bromo-2,5-dimethhoxyphenylisopropylamine ([3H]DOB), a 5-HT2 agonist radioligand. Biochem Pharmacol 36:3265–3271

    Google Scholar 

  • Tune LE, Creese I, Depaulo JR, Slavney P, Coyle JT, Snyder SH (1980) Clinical state and serum neuroleptic levels measured by radioreceptor assay in schizophrenia. Am J Psychiatry 137:187–190

    Google Scholar 

  • Wander TJ, Nelson A, Okazaki H, Richelson E (1987) Antagonism by neuroleptics of serotonin 5-HT1A receptors of normal human brain in vitro. Eur J Pharmacol 143:279–282

    Google Scholar 

  • Wong DF, Wagner HN, Tune LE, Dannals RF, Pearlson GD, Links JM, Tamminga CA, Broussolle EP, Ravert HT, Wilson AA, Toung JKT, Malat J, Williams JA, O'Tauma LA, Snyder SH, Kuhar MJ, Gedde A (1986) Positron emission tomography reveals elevated D2 dopamine receptors in drug-naive schizophrenics. Science 234:1558–1563

    Google Scholar 

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Andorn, A.C., Vittorio, J.A. & Bellflower, J. 3H-spiroperidol binding in human temporal cortex (brodmann areas 41–42) occurs at multiple high affinity states with serotonergic selectivity. Psychopharmacology 99, 520–525 (1989). https://doi.org/10.1007/BF00589902

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  • DOI: https://doi.org/10.1007/BF00589902

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