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High-Affinity Binding of Antidepressants to Platelets and Brain Tissues

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Analysis of Psychiatric Drugs

Part of the book series: Neuromethods ((NM,volume 10))

Abstract

Although antidepressant drug treatment is a well-established therapeutic approach in manic-depressive disorders, the mechanism by which such drugs ameliorate the depressive syndromes remains an area of active research. The mechanism of action of antidepressants most likely has two components. The clinical manifestation of their therapeutic effects generally is seen after a l-to 2-wk treatment, thus implying that a degree of neuronal adaptation under the effect of antidepressants is required for clinical efficacy. The development of neuronal sub-or supersensitivity following subchronic antidepressant treatment, however, is thought to be secondary to the direct interaction of these drugs with specific receptors and/or enzymes in the brain. To characterize this interaction of antidepressants with such receptors and/or enzymes, radioligand binding studies using mostly 3H-labeled antidepressants have been used extensively. Foremost among these is [3H]-imipramine, a tricyclic antidepressant that inhibits neuronal serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (noradrenaline, NA) transport. Other radiolabeled antidepressants whose high-affinity binding sites have been studied in the brain and peripheral tissues include [3H]-desipramine, [3H]-nomifensine, [3H]-indalpine, [3H]-paroxetine, [3H]-cyanoimipramine, [3H]-amitriptyline, [3H]-doxepin, [3H]-mianserin, and [3H]-rolipram (Table 1

Table 1 Antidepressants as High-Affinity Radiohgands
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Authors and Affiliations

  1. Department of Biology, LERS Synthelabo, Paris, France

    Hans Schoemaker & Salomon Z. Langer

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  1. Hans Schoemaker
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  2. Salomon Z. Langer
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  1. University of Saskatchewan, Saskatoon, Canada

    Alan A. Boulton

  2. University of Alberta, Edmonton, Canada

    Glen B. Baker  & Ronald T. Coutts  & 

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Schoemaker, H., Langer, S.Z. (1988). High-Affinity Binding of Antidepressants to Platelets and Brain Tissues. In: Boulton, A.A., Baker, G.B., Coutts, R.T. (eds) Analysis of Psychiatric Drugs. Neuromethods, vol 10. Humana Press. https://doi.org/10.1385/0-89603-121-7:429

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  • DOI: https://doi.org/10.1385/0-89603-121-7:429

  • Publisher Name: Humana Press

  • Print ISBN: 978-0-89603-121-0

  • Online ISBN: 978-1-59259-615-7

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