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New mechanisms and novel therapeutics: fresh perspectives for targeting serotonin 5-HT1A receptor function| old_uid | 11817 |
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| title | New mechanisms and novel therapeutics: fresh perspectives for targeting serotonin 5-HT1A receptor function |
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| start_date | 2012/11/15 |
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| schedule | 15h |
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| online | no |
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| location_info | 3e étage, salle de réunion |
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| details | CRNL-BIORAN "Biomarqueurs radiopharmaceutiques et neurochimiques" |
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| summary | Since the early characterization of 5-HT1A receptors in the 1980s, many efforts have been made to investigate the function of this receptor subtype. Its expression in diverse brain regions controlling mood, cognition and movement has led to the synthesis and testing of 5-HT1A agonists and antagonists drugs in various CNS indications. Until the 1990s, interest was particularly focused on the treatment of anxiety. However, several clinically-tested drugs, such as buspirone and its analogues, gave disappointing results and interest in 5-HT1A receptors faded.
Interestingly, over recent years, a series of advances in the understanding of serotonergic neurotransmission have re-launched interest in 5-HT1A receptors as a promising therapeutic target. Several clinically-employed drugs now exhibit 5-HT1A agonist properties for the treatment of a broad palette of indications, including depression (e.g. vilazodone), schizophrenia (e.g. aripiprazole) and Parkinson’s disease (e.g. pardoprunox, in clinical trials). The seminar will focus on some of the recent advances, with particular reference to treatment of depressive disorders and cognitive deficits in schizophrenia.
Notably, different brain regions exhibit distinct 5-HT1A receptor-mediated intracellular signaling cascades allowing distinct pharmacological targeting of 5?HT1A receptor subpopulations by "biased agonists", exemplified by F15599 which preferentially activates cortical 5-HT1A receptors. Such drugs offer the potential to specifically target those receptor subpopulations that mediate therapeutic properties without activating receptors in brain regions that mediate side-effects and therefore offer a novel strategy to treat pathologies involving dysfunctional serotonergic neurotransmission. |
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| responsibles | Béranger, Rossetti |
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