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NLX-112, a highly selective 5-HT(1A) receptor agonist, mediates analgesia and antidepressant-like activity in rats via spinal cord and prefrontal cortex 5-HT(1A) receptors, respectively.
Newman-Tancredi A, Bardin L, Auclair A, Colpaert F, Depoortère R, Varney MA. Newman-Tancredi A, et al. Brain Res. 2018 Jun 1;1688:1-7. doi: 10.1016/j.brainres.2018.03.016. Epub 2018 Mar 16. Brain Res. 2018. PMID: 29555239
NLX-112 (a.k.a. F13640 or befiradol) possesses marked activity in a variety of animal models of pain and of neuropsychiatric disorders; it exhibits nanomolar affinity, exceptional selectivity and high agonist efficacy at 5-hydroxytryptamine1A (
NLX-112 (a.k.a. F13640 or befiradol) possesses marked activity in a variety of animal models of pain and of neur
Antinociceptive, antiallodynic and antihyperalgesic effects of the 5-HT(1A) receptor selective agonist, NLX-112 in mouse models of pain.
Sałat K, Kołaczkowski M, Furgała A, Rojek A, Śniecikowska J, Varney MA, Newman-Tancredi A. Sałat K, et al. Neuropharmacology. 2017 Oct;125:181-188. doi: 10.1016/j.neuropharm.2017.07.022. Epub 2017 Jul 24. Neuropharmacology. 2017. PMID: 28751195
BACKGROUND AND PURPOSE: NLX-112 (a.k.a. befiradol, F13640) is a drug candidate intended for the treatment of l-DOPA-induced dyskinesia. ...The effects of NLX-112 in this test were completely abolished by the selective 5-HT(1A) rece …
BACKGROUND AND PURPOSE: NLX-112 (a.k.a. befiradol, F13640) is a drug candidate intended for the treatment of l-D …
Distinctive in vitro signal transduction profile of NLX-112, a potent and efficacious serotonin 5-HT(1A) receptor agonist.
Newman-Tancredi A, Martel JC, Cosi C, Heusler P, Lestienne F, Varney MA, Cussac D. Newman-Tancredi A, et al. J Pharm Pharmacol. 2017 Sep;69(9):1178-1190. doi: 10.1111/jphp.12762. Epub 2017 Jun 14. J Pharm Pharmacol. 2017. PMID: 28612503
OBJECTIVES: NLX-112 (befiradol, F13640) is a selective serotonin 5-HT(1A) receptor agonist. Although it has been tested in vivo, little has been reported on its in vitro signal transduction profile. METHODS: NLX-112 was tested on G …
OBJECTIVES: NLX-112 (befiradol, F13640) is a selective serotonin 5-HT(1A) receptor agonist. Although it h …
Serotonin 5-HT(1A) Receptor Biased Agonists Induce Different Cerebral Metabolic Responses: A [(18)F]-Fluorodesoxyglucose Positron Emission Tomography Study in Conscious and Anesthetized Rats.
Levigoureux E, Vidal B, Fieux S, Bouillot C, Emery S, Newman-Tancredi A, Zimmer L. Levigoureux E, et al. ACS Chem Neurosci. 2019 Jul 17;10(7):3108-3119. doi: 10.1021/acschemneuro.8b00584. Epub 2019 Jan 7. ACS Chem Neurosci. 2019. PMID: 30576601
Several 5-HT(1A) receptor biased agonists are currently in development, including NLX-101 (aka F15599) and NLX-112 (aka F13640, befiradol), with preclinical data suggesting that they preferentially target different populatio …
Several 5-HT(1A) receptor biased agonists are currently in development, including NLX-101 (aka F15599) and NL
NLX-112, a novel 5-HT1A receptor agonist for the treatment of L-DOPA-induced dyskinesia: Behavioral and neurochemical profile in rat.
Iderberg H, McCreary AC, Varney MA, Kleven MS, Koek W, Bardin L, Depoortère R, Cenci MA, Newman-Tancredi A. Iderberg H, et al. Exp Neurol. 2015 Sep;271:335-50. doi: 10.1016/j.expneurol.2015.05.021. Epub 2015 May 30. Exp Neurol. 2015. PMID: 26037043
Here, we describe the activity of a novel, highly selective and potent 5-HT1A agonist, NLX-112 (also known as befiradol or F13640) in rat models relevant to PD and its associated affective disorders. ...However, upon repeated administration of …
Here, we describe the activity of a novel, highly selective and potent 5-HT1A agonist, NLX-112 (also known as befira
The novel 5-HT1A receptor agonist, NLX-112 reduces l-DOPA-induced abnormal involuntary movements in rat: A chronic administration study with microdialysis measurements.
McCreary AC, Varney MA, Newman-Tancredi A. McCreary AC, et al. Neuropharmacology. 2016 Jun;105:651-660. doi: 10.1016/j.neuropharm.2016.01.013. Epub 2016 Jan 9. Neuropharmacology. 2016. PMID: 26777281
The highly selective and efficacious 5-HT1A receptor agonist, NLX-112 (befiradol or F13640) shows potent activity in a rat model of LID (suppression of Abnormal Involuntary Movements, AIMs) but its anti-AIMs effects have not previously been inve …
The highly selective and efficacious 5-HT1A receptor agonist, NLX-112 (befiradol or F13640) shows potent …
NLX-112, a highly selective 5-HT(1A) receptor agonist: Effects on body temperature and plasma corticosterone levels in rats.
Newman-Tancredi A, Depoortère R, Carilla-Durand E, Tarayre JP, Kleven M, Koek W, Bardin L, Varney MA. Newman-Tancredi A, et al. Pharmacol Biochem Behav. 2018 Feb;165:56-62. doi: 10.1016/j.pbb.2017.11.002. Epub 2017 Nov 7. Pharmacol Biochem Behav. 2018. PMID: 29126856
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity, exceptional selectivity and high agonist efficacy at 5-hydroxytryptamine 5-HT(1A) receptors. ...The increase in corticosterone induced by NLX-112 (0.63mg/kg
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity, exceptional selectivity and high agonist effi
Characterizing the differential roles of striatal 5-HT(1A) auto- and hetero-receptors in the reduction of l-DOPA-induced dyskinesia.
Meadows SM, Chambers NE, Conti MM, Bossert SC, Tasber C, Sheena E, Varney M, Newman-Tancredi A, Bishop C. Meadows SM, et al. Exp Neurol. 2017 Jun;292:168-178. doi: 10.1016/j.expneurol.2017.03.013. Epub 2017 Mar 23. Exp Neurol. 2017. PMID: 28342749
In experiment 2, we elucidated the role of striatal 5-HT(1A)R in the effects of F13714 and F15599. Hemi-parkinsonian, l-DOPA-primed rats received bilateral intra-striatal microinjections of either F13714 (0, 2 or 10μg/side) or F15599 (0, 10 or 3 …
In experiment 2, we elucidated the role of striatal 5-HT(1A)R in the effects of F13714 and F15599. Hemi-parkinsonian, l …
Cortical 5-hydroxytryptamine 1A receptor biased agonist, NLX-101, displays rapid-acting antidepressant-like properties in the rat chronic mild stress model.
Depoortère R, Papp M, Gruca P, Lason-Tyburkiewicz M, Niemczyk M, Varney MA, Newman-Tancredi A. Depoortère R, et al. J Psychopharmacol. 2019 Nov;33(11):1456-1466. doi: 10.1177/0269881119860666. Epub 2019 Jul 10. J Psychopharmacol. 2019. PMID: 31290370
BACKGROUND: NLX-101 (also known as F15599) is a highly selective and efficacious 'biased' agonist at cortical 5-hydroxytryptamine 1A (5-HT(1A)) heteroreceptors. ...The effects of NLX-101 were maintained over the 2 week treat …
BACKGROUND: NLX-101 (also known as F15599) is a highly selective and efficacious 'biased' agonist at cortical 5- …
In vivo biased agonism at 5-HT(1A) receptors: characterisation by simultaneous PET/MR imaging.
Vidal B, Fieux S, Redouté J, Villien M, Bonnefoi F, Le Bars D, Newman-Tancredi A, Costes N, Zimmer L. Vidal B, et al. Neuropsychopharmacology. 2018 Oct;43(11):2310-2319. doi: 10.1038/s41386-018-0145-2. Epub 2018 Jul 6. Neuropsychopharmacology. 2018. PMID: 30030540 Free PMC article.
We compared two 5-HT(1A)-biased agonists, NLX-112 and NLX-101, injected at three different doses in anaesthetised cats (n = 4). ...Functional connectivity, as measured by BOLD signal temporal correlations between regions, was also differe …
We compared two 5-HT(1A)-biased agonists, NLX-112 and NLX-101, injected at three different doses in anaes …
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