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3-Chloro-4-[18F]fluorophenyl-(4-fluoro-4-[[(5-methyl-pyrimidin-2-ylmethyl)-amino]-methyl]-piperidin-1-yl)methanone (F15599).
Leung K. Leung K. 2012 Jun 20 [updated 2012 Oct 11]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2012 Jun 20 [updated 2012 Oct 11]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 23077753 Free Books & Documents. Review.
However, none of these antagonists distinguishes between the high- and low-affinity states of the 5-HT(1A) receptors. The high-affinity state of the receptor is coupled to G-proteins, which mediate cell functions by providing intracellular signals. 2-(4-(4 …
However, none of these antagonists distinguishes between the high- and low-affinity states of the 5-HT(1A) receptors. The high-affini …
The selective 5-HT1A 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-HT1A Receptor Biased Agonists Induce Different Cerebral Metabolic Responses: A [18F]-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-HT1A 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-HT1A 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-101, a highly selective 5-HT1A receptor biased agonist, mediates antidepressant-like activity in rats via prefrontal cortex 5-HT1A receptors.
Depoortère R, Auclair AL, Newman-Tancredi A. Depoortère R, et al. Behav Brain Res. 2021 Mar 5;401:113082. doi: 10.1016/j.bbr.2020.113082. Epub 2020 Dec 25. Behav Brain Res. 2021. PMID: 33358917
NLX-101 (also known as F15599) exhibits nanomolar affinity, exceptional selectivity and biased agonist activation of serotonin 5-HT(1A) receptors. ...These data suggest that NLX-101 may target specific 5-HT(1A) receptor subpopulati …
NLX-101 (also known as F15599) exhibits nanomolar affinity, exceptional selectivity and biased agonist activation of se …
NLX-112, a highly selective 5-HT1A receptor agonist, mediates analgesia and antidepressant-like activity in rats via spinal cord and prefrontal cortex 5-HT1A 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 …
Characterizing the differential roles of striatal 5-HT1A 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
Both compounds significantly reduced LID, without affecting motor performance, however, acute administration of F13714 significantly induced 5-HT syndrome at anti-dyskinetic doses. In experiment 2, we elucidated the role of striatal 5-HT(1A)R in the effects o …
Both compounds significantly reduced LID, without affecting motor performance, however, acute administration of F13714 significantly induced …
NLX-101, a cortical 5-HT1A receptor biased agonist, reverses scopolamine-induced deficit in the delayed non-matching to position model of cognition.
Depoortere RY, Auclair AL, Newman-Tancredi A. Depoortere RY, et al. Brain Res. 2021 Aug 15;1765:147493. doi: 10.1016/j.brainres.2021.147493. Epub 2021 Apr 20. Brain Res. 2021. PMID: 33887253
NLX-101 is a selective, high efficacy, biased agonist at post-synaptic cortical 5-HT(1A) receptors. ...Moreover, NLX-101 (0.04 and 0.16 mg/kg) dose-dependently and significantly opposed scopolamine-induced impairment for 5 and 10 s delays …
NLX-101 is a selective, high efficacy, biased agonist at post-synaptic cortical 5-HT(1A) receptors. ...Moreover, NLX …
The selective 5-HT1A 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, …
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