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Agonist-Induced Down-Regulation of β1-Adrenergic Receptors: Possible Biochemical Rationale for Novel Antidepressants

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New Directions in Affective Disorders
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Abstract

Changes in the linkage between the serotonergic and noradrenergic neuronal systems at the level of the norepinephrine (NE) receptor coupled adenylate cyclase is currently the favored hypothesis to explain the mechanism of action of antidepressant drugs. In particular, the down-regulation of β-adrenoceptors (βARs), which is associated with a subsensitivity of the receptor-coupled adenylate cyclase, has been postulated as a marker of antidepressant efficacy as the time course for this action corresponds closely with the onset of clinical therapeutic effects. It has also been proposed that centrally acting βAR agonists, which interact directly with the receptor, could down-regulate βARs in the brain more quickly than classical antidepressants and would therefore cause rapid-onset antidepressant effects in patients.

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© 1989 Springer-Verlag New York Inc.

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Stahl, S.M. (1989). Agonist-Induced Down-Regulation of β1-Adrenergic Receptors: Possible Biochemical Rationale for Novel Antidepressants. In: Lerer, B., Gershon, S. (eds) New Directions in Affective Disorders. Springer, New York, NY. https://doi.org/10.1007/978-1-4612-3524-8_6

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  • DOI: https://doi.org/10.1007/978-1-4612-3524-8_6

  • Publisher Name: Springer, New York, NY

  • Print ISBN: 978-0-387-96769-1

  • Online ISBN: 978-1-4612-3524-8

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