Search Results - "DEPOORTERE, Ronan"
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The selective 5-HT1A receptor agonist NLX-112 displays anxiolytic-like activity in mice
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-02-2022)“…Anxiety is amongst the commonest neuropsychiatric disorders, and there is a large body of evidence to suggest that abnormalities in serotonergic function are…”
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Discriminative stimulus properties of the 5-HT1A receptor biased agonists NLX-101 and F13714, in rats trained to discriminate 8-OH-DPAT from saline
Published in Behavioural pharmacology (01-12-2021)“…NLX-101 and F13714 are selective, full efficacy, biased agonists of the serotonin (5-HT1A) receptor. NLX-101 preferentially activates cortical postsynaptic…”
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Multimodal imaging study of the 5-HT1A receptor biased agonist, NLX-112, in a model of L-DOPA-induced dyskinesia
Published in NeuroImage clinical (01-01-2023)“…[Display omitted] •Hemiparkinsonian (HPK) rats show a specific L-DOPA-induced brain metabolic pattern.•NLX-112 attenuated or reversed the cerebral effects of…”
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Dissecting the contribution of 5-HT1A auto- and heteroreceptors in sucrose overconsumption in mice
Published in Biomedicine & pharmacotherapy (01-04-2022)“…The rise in obesity prevalence has been linked to overconsumption of high-sugar containing food and beverages. Recent evidence suggests that chronic sucrose…”
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Translating biased agonists from molecules to medications: Serotonin 5-HT1A receptor functional selectivity for CNS disorders
Published in Pharmacology & therapeutics (Oxford) (01-01-2022)“…Biased agonism (or “functional selectivity”) at G-protein-coupled receptors has attracted rapidly increasing interest as a means to improve discovery of more…”
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Pharmacodynamic, pharmacokinetic and rat brain receptor occupancy profile of NLX-112, a highly selective 5-HT1A receptor biased agonist
Published in Naunyn-Schmiedeberg's archives of pharmacology (03-08-2024)“…NLX-112 (i.e., F13640, befiradol) exhibits nanomolar affinity, exceptional selectivity and full agonist efficacy at serotonin 5-HT1A receptors. NLX-112 shows…”
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The 5-HT1A receptor biased agonists, NLX-204 and NLX-101, display ketamine-like RAAD and anti-TRD activities in rat CMS models
Published in Psychopharmacology (01-11-2023)“…Objectives NLX-101 and NLX-204 are highly selective serotonin 5-HT 1A ‘biased’ agonists, displaying potent and efficacious antidepressant-like activity upon…”
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The 5-HT1A receptor biased agonists, NLX-204 and NLX-101, like ketamine, elicit rapid-acting antidepressant activity in the rat chronic mild stress model via cortical mechanisms
Published in Journal of psychopharmacology (Oxford) (01-07-2024)“…Background: The highly selective 5-HT1A serotonin receptor “biased” agonists NLX-101 and NLX-204 display, like ketamine, potent and efficacious rapid-acting…”
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Serotonin 5‑HT1A Receptor Biased Agonists Display Differential Anxiolytic Activity in a Rat Social Interaction Model
Published in ACS chemical neuroscience (17-07-2019)“…When placed in an unfamiliar and brightly lit open-field, two adult male rats that have not previously interacted display a low level of social interaction…”
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The 5-HT1A receptor biased agonist, NLX-204, shows rapid-acting antidepressant-like properties and neurochemical changes in two mouse models of depression
Published in Behavioural brain research (13-02-2023)“…Activation of cortical serotonin 5-HT1A receptors may be a promising strategy to achieve rapid-acting antidepressant (RAAD) activity. NLX-204 is a selective…”
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Effects of antipsychotics and reference monoaminergic ligands on marble burying behavior in mice
Published in Behavioural pharmacology (01-03-2008)“…Antipsychotics constitute efficacious augmenting agents in the treatment of anxiety disorders, including refractory obsessive-compulsive disorder. We examined…”
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Cortical 5-hydroxytryptamine 1A receptor biased agonist, NLX-101, displays rapid-acting antidepressant-like properties in the rat chronic mild stress model
Published in Journal of psychopharmacology (Oxford) (01-11-2019)“…Background: NLX-101 (also known as F15599) is a highly selective and efficacious ‘biased’ agonist at cortical 5-hydroxytryptamine 1A (5-HT1A) heteroreceptors…”
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Fentanyl dose-sparing in polyarthritic rats requires full agonism at 5-HT 1A receptors: Comparison between NLX-112, (±)8-OH-DPAT, and buspirone
Published in Journal of opioid management (01-07-2024)“…NLX-112 (a.k.a. F13640, befiradol) is a highly selective and fully efficacious agonist at 5-hydroxytryptamine (5-HT ) receptors. It has been shown to be…”
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NLX-101, a cortical 5-HT1A receptor biased agonist, reverses scopolamine-induced deficit in the delayed non-matching to position model of cognition
Published in Brain research (15-08-2021)“…•The delayed non-matching to position (DNMTP) is a model of memory/cognition.•The muscarinic antagonist, scopolamine, produces cognitive deficits in the…”
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F15599, a preferential post-synaptic 5-HT1A receptor agonist: Activity in models of cognition in comparison with reference 5-HT1A receptor agonists
Published in European neuropsychopharmacology (01-09-2010)“…Abstract We assessed the activity of F15599, a selective and high efficacy 5-HT1A agonist that preferentially activates post- versus pre-synaptic receptors, in…”
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Neural serotonergic circuits for controlling long-term voluntary alcohol consumption in mice
Published in Molecular psychiatry (01-11-2022)“…Alcohol-use-disorders are chronic relapsing illnesses, often co-morbid with anxiety. We have previously shown using the “drinking-in-the-dark” model in mice…”
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Evaluation of milnacipran, in comparison with amitriptyline, on cold and mechanical allodynia in a rat model of neuropathic pain
Published in European journal of pharmacology (25-03-2011)“…Milnacipran, a serotonin/norepinephrine reuptake inhibitor (SNRI), has shown efficacy against several chronic pain conditions, including fibromyalgia. Here, we…”
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The central serotonin2B receptor: a new pharmacological target to modulate the mesoaccumbens dopaminergic pathway activity
Published in Journal of neurochemistry (01-09-2010)“…J. Neurochem. (2010) 114, 1323–1332. The function of the serotonin2B receptor (5‐HT2BR) in the mammalian brain is poorly characterized, especially with regard…”
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Haloperidol-induced catalepsy is absent in dopamine D2, but maintained in dopamine D3 receptor knock-out mice
Published in European journal of pharmacology (01-03-2000)Get full text
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F15599, a highly selective post-synaptic 5-HT1A receptor agonist: in-vivo profile in behavioural models of antidepressant and serotonergic activity
Published in The international journal of neuropsychopharmacology (01-11-2010)“…F15599 is a novel agonist with high selectivity and efficacy at serotonin 5-HT1A receptors (5-HT1ARs). In signal transduction, electrophysiological and…”
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