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Cloning and functional expression of a Drosophila metabotropic glutamate receptor expressed in the embryonic CNS
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Albani Torregrossa S, Attucci S, Marinozzi M, Pellicciari R, Moroni F, Pellegrini-Giampietro DE: Antagonist pharmacology of metabotropic glutamate receptors coupled to phospholipase D activation in adult rat hippocampus: Focus on (2R,1′S,2′R,3′S)-2-(2′-carboxy-3′-phenylcyclopropyl)glycine versus 2,3-dihydroxyphenylglycine. Mol Pharmacol 1999, 55:699-707. The pharmacology of a new class of phospholipase D (PLD)-coupled metabotropic glutamate receptors is described. PCCG-13, a new potent, selective and competitive antagonist, the first so far described, is pharmacologically characterized and will allow a better understanding of the role played by the novel class of PLD-coupled receptors.
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O'Hara PJ, Sheppard PO, Thogersen H, Venezia D, Haldeman BA, McGrane V, Houamed KM, Thomsen C, Gilbert TL, Mulvihill ER: The ligand-binding domain in metabotropic glutamate receptors is related to bacterial periplasmic binding proteins. Neuron 1993, 11:41-52.
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Costantino G, Pellicciari R: Homology modeling of metabotropic glutamate receptors (mGluRs). Structural motifs affecting binding modes and pharmacological profile of mGluR1 agonists and competitive antagonists. J Med Chem 1996, 39:3998-4006.
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Eaton SA, Jane DE, Jones PL, Porter RH, Pook PC, Sunter DC, Udvarhelyi PM, Roberts PJ, Salt TE, Watkins JC: Competitive antagonism at metabotropic glutamate receptors by (S)-4-carboxyphenylglycine and (RS)-alpha-methyl-4-carboxyphenylglycine. Eur J Pharmacol 1993, 244:195-197.
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Pellicciari R, Luneia R, Costantino G, Marinozzi M, Natalini B, Jakobsen P, Kanstrup A, Lombardi G, Moroni F, Thomsen C: 1-Aminoindan-1,5-dicarboxylic acid: A novel antagonist at phospholipase C-linked metabotropic glutamate receptors. J Med Chem 1995, 38:3717-3719.
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(S)-(+)-2-(3′-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist
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Pellicciari R, Raimondo M, Marinozzi M, Natalini B, Costantino G, Thomsen C: (S)-(+)-2-(3′-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist. J Med Chem 1996, 39:2874-2876.
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(RS)-2-chloro-5 hydroxyphenylglycine (CHPG) activates mGlu5, but not mGlu1, receptors expressed in CHO cells and potentiates NMDA responses in the hippocampus
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Doherty AJ, Palmer MJ, Henley JM, Collingridge GL, Jane DE: (RS)-2-chloro-5 hydroxyphenylglycine (CHPG) activates mGlu5, but not mGlu1, receptors expressed in CHO cells and potentiates NMDA responses in the hippocampus. Neuropharmacology 1997, 36:265-267.
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18
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CPCOOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding
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Litschig S, Gasparini F, Rueegg D, Stoehr N, Flor PJ, Vranesic I, Prezeau L, Pin JP, Thomsen C, Kuhn R: CPCOOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding. Mol Pharmacol 1999, 55:453-461. This paper is the first to describe the possibility of modulating mGluR1 through noncompetitive antagonists.
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A novel class of antagonists for metabotropic glutamate receptors, 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylates
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Annoura H, Fukunaga A, Uesugi M, Tatsuoka T, Horikawa Y: A novel class of antagonists for metabotropic glutamate receptors, 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylates. Bioorg Med Chem Lett 1996, 6:763-767.
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0000605332
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Methylphenylethynylpiperldine (MPEP): A novel potent subtype selective and systemically active antagonist at metabotropic glutamate receptor subtype 5
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in press
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Gasparini F, Lingenheokl K, Flor PJ, Munier N, Heinrich M, Pagano A, Vranesic I, Biollaz M, Heckendorn R, Allgeier H et al.: Methylphenylethynylpiperldine (MPEP): A novel potent subtype selective and systemically active antagonist at metabotropic glutamate receptor subtype 5. Br J Pharmacol 1999, in press. This paper describes a new, potent and systemically active noncompetitive metabotropic glutamate receptor subtype 5 antagonist, the first so far reported, and highlights its anti-hyperalgesic activities.
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Br J Pharmacol
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Gasparini, F.1
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0009605613
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AIDA and S-CBPG, two mGlu1 receptor-preferring antagonists reduce neuronal death and in vivo models of cerebral ischemia
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Pellegrini-Giampietro DE, Cozzi A, Peruginelli F, Leonardi P, Meli E, Pellicciari R, Moroni F: AIDA and S-CBPG, two mGlu1 receptor-preferring antagonists reduce neuronal death and in vivo models of cerebral ischemia. Eur J Neurosci 1999, in press. This paper points out the role of metabotropic glutamate receptor subtype 1 antagonist receptors in the pathological mechanisms responsible for the postischemic neuronal death.
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Eur J Neurosci
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Pellegrini-Giampietro, D.E.1
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Presynaptic mGlu1 type receptors potentiate transmitter output in the rat cortex
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Hyperalgesia and allodynia induced by intrathecal (RS)-dihydroxyphenylglycine in rats
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Synthesis and pharmacological characterization of all sixteen stereoisomers of 2-(2′-carboxy-3′-phenylcyclopropylglycine. Focus on (2S,1′S,2′S,3′R-2-(2′-carboxy-3′-phenylcyclopropyl)glycine, a novel and selective group II metabotropic glutamate receptors antagonist
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Pellicciari R, Marinozzi M, Natalini B, Costantino G, Luneia R, Giorgi G, Moroni F, Thomsen C: Synthesis and pharmacological characterization of all sixteen stereoisomers of 2-(2′-carboxy-3′-phenylcyclopropyl)glycine. Focus on (2S,1′S,2′S,3′R)-2-(2′-carboxy-3′-phenylcyclopropyl)glycine, a novel and selective group II metabotropic glutamate receptors antagonist. Med Chem 1996, 39:2259-2269.
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Kozikowski AP, Steensma D, Araldi GL, Tuckmantel W, Wang S, Pshenichkin S, Surina E, Wroblewski JT: Synthesis and biology of the conformationally restricted ACPD analogue, 2-aminobicyclo[2.1.1]hexane-2,5-dicarboxylic acid-l, a potent mGluR agonist. J Med Chem 1998, 41:1641-1650. The synthesis and the biological evaluation of a new conformationally constrained ⌊-glutamate analog, eqiupotent as a metabotropic glutamate receptor subtype 1 and 2 agonist, is reported. Very interesting structure/activity relationships are shown.
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Monn JA, Valli MJ, Massey SM, Wright RA, Salhoff CR, Johnson BG, Howe T, Alt CA, Rhodes GA, Robey RL et al.: Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): A potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties. J Med Chem 1997, 40:528-537.
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Monn JA, Valli MJ, Massey SM, Hansen MM, Kress TJ, Wepsiec JP, Harkness AR, Grutsch JL Jr, Wright RA, Johnson BG et al.: Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic ammo acids related to (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): Identification of two new potent, selective, and systemically active agonists for group II metabotropic glutamate receptors. J Med Chem 1999, 42:1027-1040.
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Type 2 metabotropic glutamate (mGlu) receptors tonically inhibit transmitter release in rat caudate nucleus: In vivo studies with (2S,1′S,2′S,3′R-2-(2′-carboxy-3′-phenylcyclopropyl)glycine, a new potent and selective antagonist
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Cozzi A, Attucci S, Peruginelli F, Marinozzi M, Luneia R, Pellicciari R, Moroni F: Type 2 metabotropic glutamate (mGlu) receptors tonically inhibit transmitter release in rat caudate nucleus: In vivo studies with (2S,1′S,2′S,3′R)-2-(2′-carboxy-3′-phenylcyclopropyl)glycine, a new potent and selective antagonist. Eur J Neurosci 1997, 9:1350-1355.
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Moghaddam B, Adams BW: Reversal of phencyclidine effects by a group II metabotropic glutamate receptor agonist in rats. Science 1998, 281:1349-1352. The therapeutic potential of group II agonists in the treatment of psychiatric disorders such as schizophrenia is described in this paper. LY354740 is shown to reverse the effect of phenyciclidine in rats, a common experimental model for epilepsy.
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