2-Methyl-6-(phenylethynyl)-pyridine (MPEP), a potent, selective and systemically active mGlu5 receptor antagonist

Annoura, H., Fukunaga, A., Vesugi, M., Tatsuoku, T., Horikawa, Y., 1996. A novel class of antagonists for metabotropic glutamate receptors, 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylates. Bioorganic Med. Chem Letters. 6, 763–766.

Baker, R., Clark, B.P., Harris, J.R., Griffey, K.I., Kingston, A.E., Tizzano, J.P., 1998. LY393675, an a-substituted-cyclobutylglycine, is a potent group I metabotropic glutamate receptor antagonist. Soc. Neurosci. Abstr. 229.16.

Birse, 1993, Phenylglycine derivatives as new pharmacological tools for investigating the role of metabotropic glutamate receptors in the central nervous system, Neuroscience, 52, 481, 10.1016/0306-4522(93)90400-A

Bowes, M., Panesar, M., Gentry, C., et al., 1999. Anti-hyperalgesic effects of the novel metabotropic glutamate receptor 5 antagonist, methylphenylethynylpyridine, in rat models of inflammatory pain. Br. J. Pharm. (in press).

Charpak, 1990, Potassium conductances in hippocampal neurons blocked by excitatory amino acid transmitters, Nature, 347, 765, 10.1038/347765a0

Communi, 1997, Receptors responsive to extracellular pyridine nucleotides, TiPS, 18, 83

Conn, 1997, Pharmacology and functions of metabotropic glutamate receptors, Annu. Rev. Pharmacol. Toxicol., 37, 205, 10.1146/annurev.pharmtox.37.1.205

Daggett, 1995, Molecular and functional characterization of recombinant human glutamate receptor subtype 5, Neuropharmacology, 34, 871, 10.1016/0028-3908(95)00085-K

Daggett, L.P., Jachec, C., Lin, F.F., et al., 1996. Functional characterization of two isoforms of the human GluR6 receptor and distribution of GluR6 RNA editing sites. Soc. Neurosci. Abstr. 236.11.

Desai, 1991, Excitatory effects of ACPD receptor activation in the hippocampus are mediated by direct effects on pyramidal cells and blockade of synaptic inhibition, J. Neurophys., 66, 40, 10.1152/jn.1991.66.1.40

Doherty, 1997, (R,S)-2-Chloro-5-hydroxyphenylglycine (CHPG) activates mGlu5, but not mGlu1, receptors expressed in CHO cells and potentiates NMDA responses in the hippocampus, Neuropharmacology, 36, 265, 10.1016/S0028-3908(97)00001-4

Flor, 1997, A novel splice variant of a metabotropic glutamate receptor, human mGluR7b, Neuropharmacology, 36, 1532, 10.1016/S0028-3908(96)00176-1

Flor, P.J., Bruno, V., Battaglia, G., et al., 1998. Neuroprotection in vitro and in vivo by (R,S)-PPG, a potent and selective group III metabotropic glutamate receptor agonist. Soc. Neurosci. Abstr. 431.11.

Gasparini, 1999, (R,S)-4-Phosphophenylglycine, a potent and selective group III metabotropic glutamate receptor agonist is anticonvulsive and neuroprotective in vivo, J. Pharmacol. Exp. Ther., 290, 1678

Gasparini, F., Lingenhoehl, K., Flor, P.J., et al., 1999b. Methylphenylethynylpyridine (MPEP): a novel potent, subtype-selective and systemically active antagonist at metabotropic glutamate receptor subtype 5. Br. J. Pharm. (in press).

Gereau IV, 1995, Multiple presynaptic metabotropic glutamate receptors modulate excitatory and inhibitory synaptic transmission in hippocampal area CA1, J. Neurosci., 15, 6879, 10.1523/JNEUROSCI.15-10-06879.1995

Hermans, 1998, Reversible and non-competitive antagonist profile of CPCCOEt at the human type 1a metabotropic glutamate receptor, Neuropharmacology, 12, 1645, 10.1016/S0028-3908(98)00132-4

Hess, 1996, Cloning and functional characterization of human heteromeric N-methyl-d-aspartate receptors, J. Pharmacol. Exp. Ther., 278, 808

Hollmann, 1991, Ca2+ permeability of KA-AMPA-gated glutamate receptor channels depends on subunit composition, Science, 252, 851, 10.1126/science.1709304

Ito, 1992, 3,5-Dihydroxyphenylglycine: a potent agonist of metabotropic glutamate receptors, NeuroReport, 3, 1013, 10.1097/00001756-199211000-00017

Knöpfel, 1995, Metabotropic glutamate receptors: novel targets for drug development, J. Med. Chem., 38, 1417, 10.1021/jm00009a001

Knöpfel, 1995, Profiling of trans-azetidine-2,4-dicarboxylic acid at the human metabotropic glutamate receptors mGlu1b, -2, -4a and -5a, Eur. J. Pharmacol., 288, 389, 10.1016/0922-4106(95)90054-3

Laurie, 1995, Ligand binding profile of the rat metabotropic glutamate receptor mGluR3 expressed in a transfected cell line, Naunyn Schmiedebergs Arch. Pharmacol., 351, 565, 10.1007/BF00171050

Laurie, 1997, Cloning, distribution and functional expression of the human mGlu6 metabotropic glutamate receptor, Neuropharmacology, 36, 145, 10.1016/S0028-3908(96)00172-4

Lazareno, 1993, Pharmacological characterization of guanine nucleotide exchange reactions in membranes from CHO cells stably transfected with human muscarinic receptors m1-m4, Life Sci., 52, 449, 10.1016/0024-3205(93)90301-I

Lin, 1997, Cloning and stable expression of the mGluR1b subtype of human metabotropic receptors and pharmacological comparison with the mGluR5a subtype, Neuropharmacology, 36, 917, 10.1016/S0028-3908(97)00078-6

Lingenhöhl, 1998, Reevaluation of ACEA1021 as an antagonist at the strychnine-insensitive glycine site of the N-methyl-d-aspartate receptor, Neuropharmacology, 37, 729, 10.1016/S0028-3908(98)00062-8

Litschig, 1999, CPCCOEt, a non-competitive mGluR1 antagonist, inhibits receptor signaling without affecting glutamate binding, Mol. Pharmacol., 55, 453

Liu, 1993, Activation of metabotropic glutamate receptors induces long-term depression of GABAergic inhibition in the hippocampus, J. Neurophys., 69, 1000, 10.1152/jn.1993.69.3.1000

Martin, 1992, Cellular localization of a metabotropic glutamate receptor in rat brain, Neuron, 9, 259, 10.1016/0896-6273(92)90165-A

Nicoletti, 1997, Metabotropic glutamate receptors: a new target for the therapy of neurodegenerative disorders?, TiNS, 19, 267

Pellicciari, R., Raimondo, M., Marinozzi, Natalini, B., Costantino, G., Thomsen, C., 1996. (S)-(+)-2-(3′-carboxybicyclo[1.1.1]pentyl)glycine, a structurally new groupI metabotropic glutamate receptor antagonist. J. Med. Chem. 39, 2874–2876.

Romano, 1995, Distribution of metabotropic glutamate receptor mGluR5 immunoreactivity in rat brain, J. Comp. Neurol., 355, 455, 10.1002/cne.903550310

Romano, 1996, Enhanced early developmental expression of the metabotropic glutamate receptor mGluR5 in the rat brain: protein, mRNA splice variants, and regional distribution, J. Comp. Neurol., 367, 403, 10.1002/(SICI)1096-9861(19960408)367:3<403::AID-CNE6>3.0.CO;2-9

Sacaan, 1998, (S)-4-carboxy-3-hydroxyphenylglycine activates phosphatidyl inositol linked metabotropic glutamate receptors: differential effects in neonatal rat brain regions, Neurochem. Int., 32, 77, 10.1016/S0197-0186(97)00060-0

Sashida, 1988, Thermal rearrangements of cyclic amine ylides. VIII. Intramolecular cyclization of 2-ethynylpyridine N-ylides into indolizines and cycl[3.2.2]azines, Chem. Pharm. Bull., 36, 3826, 10.1248/cpb.36.3826

Schoepp, 1994, 3,5-Dihydroxyphenylglycine is a highly selective agonist for phosphoinositide-linked metabotropic glutamate receptors in the rat hippocampus, J. Neurochem., 63, 769, 10.1046/j.1471-4159.1994.63020769.x

Sekiyama, 1996, Structure-activity relationships of new agonists and antagonists of different metabotropic glutamate receptor subtypes, Br. J. Pharmacol., 117, 1493, 10.1111/j.1476-5381.1996.tb15312.x

Shigemoto, 1993, Immunohistochemical localization of a metabotropic glutamate receptor, mGluR5 in the brain, Neurosci. Lett., 163, 53, 10.1016/0304-3940(93)90227-C

Shigemoto, 1997, Differential presynaptic localization of metabotropic glutamate receptor subtypes in the rat hippocampus, J. Neurosci., 17, 7503, 10.1523/JNEUROSCI.17-19-07503.1997

Storm, 1993, Functional diversity of K+ currents in hippocampal pyramidal neurons, Semin. Neurosci., 5, 79, 10.1016/S1044-5765(05)80002-8

Thomas, N.K., Woolley, M.L., Miller, J.C., et al., 1998. Novel phenylglycines as metabotropic glutamate receptor antagonist. Soc. Neurosci. Abstr. 229.15.

Varney, M.A., Cosford, N., Jachec, C., et al., 1999. Characterization of SIB-1757 and SIB-1893: highly selective antagonists at metabotropic glutamate receptor subtype 5. Br. J. Pharm. (in press).

Veliçelebi, 1998, Fluorescence techniques for measuring ion channel activity, Meth. Enzymol., 294, 20, 10.1016/S0076-6879(99)94005-3

Watkins, 1994, Phenylglycine derivatives as antagonists of metabotropic glutamate receptors, Trends Pharmacol. Sci., 15, 333, 10.1016/0165-6147(94)90028-0