ArticleBritish journal of pharmacology2006
Rapid desensitization of somatodendritic 5-HT1A receptors by chronic administration of the high-efficacy 5-HT1A agonist, F13714: a microdialysis study in the rat.
Article in British journal of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 61 citations in OpenAlex.
- Pharmacology of ayahuasca administered in two repeated doses.Psychopharmacology · 2012Trial
- Validation of the forced swim test in Drosophila, and its use to demonstrate psilocybin has long-lasting antidepressant-like effects in flies.Scientific reports · 2022Article
- Selective Targeting of Serotonin 5-HT1a and 5-HT3 Receptors Attenuates Acute and Long-Term Hypersensitivity Associated With Neonatal Procedural Pain.Frontiers in pain research (Lausanne, Switzerland) · 2022Article
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- Exploring the impact of trauma type and extent of exposure on posttraumatic alterations in 5-HT1A expression.Translational psychiatry · 2020Review
- Pharmacological Studies on the Role of 5-HTFrontiers in behavioral neuroscience · 2020Article
- Lurasidone Sub-Chronically Activates Serotonergic Transmission via Desensitization of 5-HT1A and 5-HT7 Receptors in Dorsal Raphe Nucleus.Pharmaceuticals (Basel, Switzerland) · 2019Article
- Cognitive impairment in depression: recent advances and novel treatments.Neuropsychiatric disease and treatment · 2019Review
- Effects of the Serotonin 5-HTNeurochemical research · 2018Article
- Marmoset Serotonin 5-HT1A Receptor Mapping with a Biased Agonist PET Probe 18F-F13714: Comparison with an Antagonist Tracer 18F-MPPF in Awake and Anesthetized States.The international journal of neuropsychopharmacology · 2016Article
- Selective serotonin 5-HT1A receptor biased agonists elicitdistinct brain activation patterns: a pharmacoMRI study.Scientific reports · 2016Article
- Anti-aggressive effects of the selective high-efficacy 'biased' 5-HT₁A receptor agonists F15599 and F13714 in male WTG rats.Psychopharmacology · 2016Article
- Functional Selectivity and Antidepressant Activity of Serotonin 1A Receptor Ligands.International journal of molecular sciences · 2015Review
- Divergent effects of the 'biased' 5-HT1 A receptor agonists F15599 and F13714 in a novel object pattern separation task.British journal of pharmacology · 2015Article
- New hypothesis and treatment targets of depression: an integrated view of key findings.Neuroscience bulletin · 2015Review
- The role of the serotonin receptor subtypes 5-HT1A and 5-HT7 and its interaction in emotional learning and memory.Frontiers in pharmacology · 2015Review
- In vivo electrophysiological and neurochemical effects of the selective 5-HT1A receptor agonist, F13640, at pre- and postsynaptic 5-HT1A receptors in the rat.Psychopharmacology · 2012Article
- Differential effects of serotonin 5-HT1A receptor agonists on the discriminative stimulus effects of the 5-HT2A receptor agonist 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane in rats and rhesus monkeys.The Journal of pharmacology and experimental therapeutics · 2010Article
- Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist.British journal of pharmacology · 2009Article
- Activation of 5-HT1A autoreceptors in the dorsal raphe nucleus reduces the behavioral consequences of social defeat.Psychoneuroendocrinology · 2008Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeDesensitization of somatodendritic 5-HT(1A) receptors is involved in the mechanism of action of several antidepressants, but the rapidity of this effect and the amount of agonist stimulation needed are unclear. We evaluated the capacity of the high-efficacy 5-HT(1A) agonist, F13714 (3-chloro-4-fluorophenyl-(4-fluoro-4-{[(5-methyl-6-methylamino-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1-yl-methanone) and of the partial agonist, flesinoxan, to desensitize somatodendritic 5-HT(1A) receptors involved in the control of 5-HT release. EXPERIMENTAL APPROACH: Intracerebral microdialysis in the hippocampus of freely moving rats was used to examine the acute and chronic effects of the two compounds (administered by osmotic pumps for 3, 7 or 14 days) on extracellular 5-HT levels, measured by HPLC with electrochemical detection. KEY
resultsWhen given acutely, F13714, flesinoxan and the low-efficacy 5-HT(1A) agonist, buspirone, dose-dependently decreased extracellular 5-HT concentrations (ED(50) values: 0.04, 0.77 and 5.6 mg kg(-1), respectively). The selective 5-HT(1A) antagonist WAY100635 inhibited the effects of the three compounds. F13714 (2.5 mg kg(-1) per day for 3, 7 or 14 days and 0.63 mg kg(-1) for 7 days) significantly attenuated the inhibition of 5-HT release induced by buspirone (10 mg kg(-1)). In contrast, flesinoxan (10 mg kg(-1) per day) failed to alter the response to buspirone at any of the treatment durations. CONCLUSIONS AND IMPLICATIONS: Rat somatodendritic 5-HT(1A) receptors controlling hippocampal 5-HT release were rapidly desensitized by chronic activation with a high-efficacy 5-HT(1A) agonist, but not by chronic activation with a partial agonist. Thus, rapid 5-HT(1A) autoreceptor desensitization by high-efficacy agonists may accelerate the onset of the therapeutic effects of antidepressants.
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