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2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist.
Gasparini F, Lingenhöhl K, Stoehr N, Flor PJ, Heinrich M, Vranesic I, Biollaz M, Allgeier H, Heckendorn R, Urwyler S, Varney MA, Johnson EC, Hess SD, Rao SP, Sacaan AI, Santori EM, Veliçelebi G, Kuhn R. Gasparini F, et al. Among authors: vranesic i. Neuropharmacology. 1999 Oct;38(10):1493-503. doi: 10.1016/s0028-3908(99)00082-9. Neuropharmacology. 1999. PMID: 10530811
The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors.
Pagano A, Ruegg D, Litschig S, Stoehr N, Stierlin C, Heinrich M, Floersheim P, Prezèau L, Carroll F, Pin JP, Cambria A, Vranesic I, Flor PJ, Gasparini F, Kuhn R. Pagano A, et al. Among authors: vranesic i. J Biol Chem. 2000 Oct 27;275(43):33750-8. doi: 10.1074/jbc.M006230200. J Biol Chem. 2000. PMID: 10934211 Free article.
Metabotropic glutamate receptor subtype 5 (mGlu5) and nociceptive function. I. Selective blockade of mGlu5 receptors in models of acute, persistent and chronic pain.
Walker K, Bowes M, Panesar M, Davis A, Gentry C, Kesingland A, Gasparini F, Spooren W, Stoehr N, Pagano A, Flor PJ, Vranesic I, Lingenhoehl K, Johnson EC, Varney M, Urban L, Kuhn R. Walker K, et al. Among authors: vranesic i. Neuropharmacology. 2001;40(1):1-9. doi: 10.1016/s0028-3908(00)00113-1. Neuropharmacology. 2001. PMID: 11077065
Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III.
Amori L, Costantino G, Marinozzi M, Pellicciari R, Gasparini F, Flor PJ, Kuhn R, Vranesic I. Amori L, et al. Among authors: vranesic i. Bioorg Med Chem Lett. 2000 Jul 3;10(13):1447-50. doi: 10.1016/s0960-894x(00)00247-x. Bioorg Med Chem Lett. 2000. PMID: 10888329
Regional brain mGlu5 receptor occupancy following single oral doses of mavoglurant as measured by [11C]-ABP688 PET imaging in healthy volunteers.
Streffer J, Treyer V, Buck A, Ametamey SM, Blagoev M, Maguire RP, Gautier A, Auberson YP, Schmidt ME, Vranesic IT, Gomez-Mancilla B, Gasparini F. Streffer J, et al. Among authors: vranesic it. Neuroimage. 2021 Apr 15;230:117785. doi: 10.1016/j.neuroimage.2021.117785. Epub 2021 Feb 2. Neuroimage. 2021. PMID: 33545349 Free article.
30 results