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The selective 5-HT(1A) receptor agonist, NLX-112, exerts anti-dyskinetic effects in MPTP-treated macaques.
Depoortere R, Johnston TH, Fox SH, Brotchie JM, Newman-Tancredi A. Depoortere R, et al. Parkinsonism Relat Disord. 2020 Sep;78:151-157. doi: 10.1016/j.parkreldis.2020.08.009. Epub 2020 Aug 13. Parkinsonism Relat Disord. 2020. PMID: 32846366
METHODS: The effects of NLX-112 (0.03, 0.1 and 0.3 mg/kg PO) on established LID evoked by acute challenge with l-DOPA (27.5 3.8 mg/kg PO) were assessed in MPTP-treated cynomolgus macaques. Amantadine (10 mg/kg PO) was tested as a positive …
METHODS: The effects of NLX-112 (0.03, 0.1 and 0.3 mg/kg PO) on established LID evoked by acute challenge with l …
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 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 …
Pharmacological MRI to investigate the functional selectivity of 5-HT(1A) receptor biased agonists.
Vidal B, Bolbos R, Redouté J, Langlois JB, Costes N, Newman-Tancredi A, Zimmer L. Vidal B, et al. Neuropharmacology. 2020 Aug 1;172:107867. doi: 10.1016/j.neuropharm.2019.107867. Epub 2019 Nov 26. Neuropharmacology. 2020. PMID: 31783063
The cerebral blood oxygen level dependent (BOLD) signal changes induced by increasing doses of two serotonin 5-HT(1A) receptor biased agonists, NLX-112 and NLX-101, were mapped in anaesthetized rats. ...Importantly, NLX-101 had no …
The cerebral blood oxygen level dependent (BOLD) signal changes induced by increasing doses of two serotonin 5-HT(1A) receptor biased …
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 …
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. ...In microdialysis experiments, NLX- …
Here, we describe the activity of a novel, highly selective and potent 5-HT1A agonist, NLX-112 (also known as befira …
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. ...NLX-112 was also tested on G-protein activation in rat hippocampal membranes. ...
OBJECTIVES: NLX-112 (befiradol, F13640) is a selective serotonin 5-HT(1A) receptor agonist. ...NLX …
The selective 5-HT(1A) receptor agonist, NLX-112, exerts anti-dyskinetic and anti-parkinsonian-like effects in MPTP-treated marmosets.
Fisher R, Hikima A, Morris R, Jackson MJ, Rose S, Varney MA, Depoortere R, Newman-Tancredi A. Fisher R, et al. Neuropharmacology. 2020 May 1;167:107997. doi: 10.1016/j.neuropharm.2020.107997. Epub 2020 Feb 10. Neuropharmacology. 2020. PMID: 32057799 Free PMC article.
Reducing the activity of these neurons diminishes l-DOPA-induced dyskinesia (LID), but there are currently no clinically approved selective, high efficacy 5-HT(1A) receptor agonists. Here we describe the effects of NLX-112, a highly selective and efficacious …
Reducing the activity of these neurons diminishes l-DOPA-induced dyskinesia (LID), but there are currently no clinically approved selective, …
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
This is likely due to conversion of l-DOPA to dopamine as a 'false neurotransmitter' from serotoninergic neurons. The highly selective and efficacious 5-HT1A receptor agonist, NLX-112 (befiradol or F13640) shows potent activity in a rat model of …
This is likely due to conversion of l-DOPA to dopamine as a 'false neurotransmitter' from serotoninergic neurons. The highly selective and e …
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- …
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