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Differential Regulation of Dopamine-D2 and Serotonin-S2 Receptors by Chronic Treatment with the Serotonin-S2 Antagonists, Ritanserin, and Setoperone

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Clinical Pharmacology in Psychiatry

Part of the book series: Psychopharmacology Series ((PSYCHOPHARM,volume 3))

Abstract

Serotonin-S2 receptor sites were first described in studies in which 3H-spiperone was used in frontal cortical membrane preparations (Leysen et al. 1978; Peroutka and Snyder 1979). The receptor binding sites were further characterized and could be better distinguished by using the more selective serotonin antagonist 3H-ke-tanserin (Leysen et al. 1982). Serotonin-S2 receptors were shown to have a role in serotonin agonist-induced behavioral excitation and discriminative stimulus effects in rodents, and also to mediate serotonin-induced vasoconstriction and platelet function. Recently it has been shown that inositol phospholipid turnover forms part of the signal transducing system coupled to serotonin-S2 receptor sites (for review see Leysen et al. 1984).

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References

  • Blackshear MA, Sanders-Bush E (1982) Serotonin receptor sensitivity after acute and chronic treatment with mianserin. J Pharmacol Exp Ther 221: 303–308

    PubMed  CAS  Google Scholar 

  • Blackshear MA, Friedman RL, Sanders-Bush E (1983) Acute and chronic effects of serotonin (5-HT) antagonists on serotonin binding sites. Naunyn-Schmiedebergs Arch Pharmacol 324: 125–129

    Article  PubMed  CAS  Google Scholar 

  • Ceulemans DLS, Gelders YG, Hoppenbrouwers MLJA, Reyntjens ASM, Janssen PAJ (1985) Effect of serotonin antagonism in schizophrenia: a pilot study with setoperone. Psychopharmacology (Berlin) 85: 329–339

    Article  CAS  Google Scholar 

  • Colpaert FC, Meert TF, Niemegeers CJE, Janssen PAJ (1985) Behavioral and 5-HT antagonist effects of ritanserin: a pure and selective antagonist of LSD discrimination in rat. Psychopharmacology (Berlin) 86: 45–54

    Article  CAS  Google Scholar 

  • Crews FT, Scott JA, Shorstein NH (1983) Rapid down-regulation of serotonin-S2 receptor binding during combined administration of tricyclic antidepressant drugs and a2 antagonists. Neuropharmacology 22: 1203–1209

    Article  PubMed  CAS  Google Scholar 

  • Gandolfi O, Barbaccia ML, Costa E (1984) Comparison of iprindole, imipramine and mianserin action on brain serotonergic and beta adrenergic receptors. J Pharmacol Exp Ther 229: 782–876

    PubMed  CAS  Google Scholar 

  • Gandolfi O, Barbaccia ML, Costa E (1985) Different effects of serotonin antagonists on 3H- mianserin and 3H-ketanserin recognition sites. Life Sci 36: 713–721

    Article  PubMed  CAS  Google Scholar 

  • Hall H, Ross SB, Sallemark M (1984) Effect of destruction of central noradrenergic and serotonergic nerve terminals by systemic neurotoxins on the long-term effects of antidepressants on β-adrenoceptors and 5-HT2 binding sites in the rat cerebral cortex. J Neural Transm 59: 9–23

    Article  PubMed  CAS  Google Scholar 

  • Hyttel J, Fredericson Overø K, Arnt J (1984) Biochemical effects and drug levels in rats after long-term treatment with the specific 5-HT-uptake inhibitor, citalopram. Psychopharmacology (Berlin) 83:20–27z8

    Google Scholar 

  • Laduron PM, Janssen PFM, Leysen JE (1982) In vivo binding of [3H]ketanserin on serotonin-S2 receptors in rat brain. Eur J Pharmacol 81: 43–48

    Article  PubMed  CAS  Google Scholar 

  • Leysen JE, Niemegeers CJE, Tollenaere JP, Laduron PM (1978) Serotonergic component of neuroleptic receptors. Nature 272: 168–171

    Article  PubMed  CAS  Google Scholar 

  • Leysen JE, Niemegeers CJE, Van Nueten JM, Laduron PM (1982) [3H]Ketanserin (R 41468),

    Google Scholar 

  • a selective 3H-ligand for serotonin2 receptor binding sites. Mol Pharmacol 21:301–314

    Google Scholar 

  • Leysen JE, de Chaffoy de Courcelles D, De Clerck F, Niemegeers CJE, Van Nueten JM (1984) Serotonin-S2 receptor binding sites and functional correlates. Neuropharmacology 23: 1493–1501

    Google Scholar 

  • Leysen JE, Gommeren W, Van Gompel P, Wynants J, Jansen PFM, Laduron PM (1985 a) Receptor-binding properties in vitro and in vivo of ritanserin. A very potent and long-acting serotonin-S2 antagonist. Mol Pharmacol 27: 600–611

    Google Scholar 

  • Leysen JE, Van Gompel P, Gommeren W, Woestenborghs R, Janssen PAJ (1986) Down regulation of serotonin-S2 receptor sites in rat brain by chronic treatment with the serotonin-S2 antagonists: ritanserin and setoperone. Psychopharmacology (Berlin) 88: 434–444

    Article  CAS  Google Scholar 

  • Niemegeers CJE, Leysen JE, Laduron PM, Janssen PAJ (1984) Differential pharmacological and biochemical profiles of serotonin-S2 antagonists. Collegium Internationale Neuro-Psychopharmacologicum, 14th Congress, 16–19 June, Firenze, pp 889 (Abstracts)

    Google Scholar 

  • Peroutka SJ, Snyder SH (1979) Multiple serotonin receptors differential binding of [3H] 5-hy-droxytryptamine, [3H] lysergic acid diethylamide, and [3H] spiroperidol. Mol Pharol 16: 687–699

    CAS  Google Scholar 

  • Peroutka SJ, Snyder SH (1980) Regulation of serotonin2 (5-HT2) receptors labeled with [3H] ;spiroperidol by chronic treatment with the antidepressant amitriptyline. J Pharmacol Exp Ther 215: 582–587

    PubMed  CAS  Google Scholar 

  • Reyntjens A, Waelkens J, Gelders Y, Ceulemans D, Janssen PAJ (1984) A novel approach for psychosomatic normalization: a placebo-controlled pilot trial of R 55 667, a potent indolamine antagonist. Collegium Internationale Neuro-Psychopharmacologicum, 14th Congress, 16–19 June, Firenze, pp 566 (Abstracts)

    Google Scholar 

  • Snyder SH, Peroutka SJ (1982) A possible role of serotonin receptors in antidepressant drug action. Pharmacopsychiatry 15: 131–134

    Article  CAS  Google Scholar 

  • Stolz JF, Marsden CA, Middlemiss DN (1983) Effect of chronic antidepressant treatment and subsequent withdrawal on [3H]5-hydroxytryptamine and [3H]spiperone binding in rat frontal cortex and serotonin receptor-mediated behaviour. Psychopharmacology (Berlin) 80: 150–155

    Article  CAS  Google Scholar 

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© 1987 Springer-Verlag Berlin Heidelberg

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Leysen, J.E., van Gompel, P., Gommeren, W., Laduron, P.M. (1987). Differential Regulation of Dopamine-D2 and Serotonin-S2 Receptors by Chronic Treatment with the Serotonin-S2 Antagonists, Ritanserin, and Setoperone. In: Dahl, S.G., Gram, L.F., Paul, S.M., Potter, W.Z. (eds) Clinical Pharmacology in Psychiatry. Psychopharmacology Series, vol 3. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-71288-3_25

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  • DOI: https://doi.org/10.1007/978-3-642-71288-3_25

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-71290-6

  • Online ISBN: 978-3-642-71288-3

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