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Chemical Compound Review

MPEP     2-methyl-6-(2- phenylethynyl)pyridine

Synonyms: Lopac-M-5435, Tocris-1212, CHEMBL66654, AC1MHGB1, SureCN103061, ...
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Disease relevance of Lopac-M-5435


Psychiatry related information on Lopac-M-5435


High impact information on Lopac-M-5435


Biological context of Lopac-M-5435


Anatomical context of Lopac-M-5435


Associations of Lopac-M-5435 with other chemical compounds


Gene context of Lopac-M-5435


Analytical, diagnostic and therapeutic context of Lopac-M-5435


  1. Reduced stress-induced hyperthermia in mGluR5 knockout mice. Brodkin, J., Bradbury, M., Busse, C., Warren, N., Bristow, L.J., Varney, M.A. Eur. J. Neurosci. (2002) [Pubmed]
  2. Selective blockade of mGlu5 metabotropic glutamate receptors is protective against methamphetamine neurotoxicity. Battaglia, G., Fornai, F., Busceti, C.L., Aloisi, G., Cerrito, F., De Blasi, A., Melchiorri, D., Nicoletti, F. J. Neurosci. (2002) [Pubmed]
  3. Metabotropic glutamate subtype 5 receptors modulate locomotor activity and sensorimotor gating in rodents. Kinney, G.G., Burno, M., Campbell, U.C., Hernandez, L.M., Rodriguez, D., Bristow, L.J., Conn, P.J. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  4. A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Hemstapat, K., de Paulis, T., Chen, Y., Brady, A.E., Grover, V.K., Alagille, D., Tamagnan, G.D., Conn, P.J. Mol. Pharmacol. (2006) [Pubmed]
  5. The mGluR5 antagonist 6-methyl-2-(phenylethynyl)pyridine decreases ethanol consumption via a protein kinase C epsilon-dependent mechanism. Olive, M.F., McGeehan, A.J., Kinder, J.R., McMahon, T., Hodge, C.W., Janak, P.H., Messing, R.O. Mol. Pharmacol. (2005) [Pubmed]
  6. Metabotropic glutamate receptor subtypes as targets for neuroprotective drugs. Bruno, V., Battaglia, G., Copani, A., D'Onofrio, M., Di Iorio, P., De Blasi, A., Melchiorri, D., Flor, P.J., Nicoletti, F. J. Cereb. Blood Flow Metab. (2001) [Pubmed]
  7. Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP. Malherbe, P., Kratochwil, N., Mühlemann, A., Zenner, M.T., Fischer, C., Stahl, M., Gerber, P.R., Jaeschke, G., Porter, R.H. J. Neurochem. (2006) [Pubmed]
  8. Substituent effects of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides on positive allosteric modulation of the metabotropic glutamate-5 receptor in rat cortical astrocytes. de Paulis, T., Hemstapat, K., Chen, Y., Zhang, Y., Saleh, S., Alagille, D., Baldwin, R.M., Tamagnan, G.D., Conn, P.J. J. Med. Chem. (2006) [Pubmed]
  9. Zinc inhibition of group I mGluR-mediated calcium homeostasis in auditory neurons. Zirpel, L., Parks, T.N. J. Assoc. Res. Otolaryngol. (2001) [Pubmed]
  10. Mouse hepatocytes lacking mGlu5 metabotropic glutamate receptors are less sensitive to hypoxic damage. Storto, M., Battaglia, G., Gradini, R., Bruno, V., Nicoletti, F., Vairetti, M. Eur. J. Pharmacol. (2004) [Pubmed]
  11. Metabotropic glutamate receptors differentially regulate GABAergic inhibition in thalamus. Govindaiah, G., Cox, C.L. J. Neurosci. (2006) [Pubmed]
  12. Modulation of the neuronal dopamine transporter activity by the metabotropic glutamate receptor mGluR5 in rat striatal synaptosomes through phosphorylation mediated processes. Page, G., Peeters, M., Najimi, M., Maloteaux, J.M., Hermans, E. J. Neurochem. (2001) [Pubmed]
  13. Effect of the mGluR5 antagonist 6-methyl-2-(phenylethynyl)pyridine (MPEP) on the acute locomotor stimulant properties of cocaine, D-amphetamine, and the dopamine reuptake inhibitor GBR12909 in mice. Mcgeehan, A.J., Janak, P.H., Olive, M.F. Psychopharmacology (Berl.) (2004) [Pubmed]
  14. Neuroprotective action of MPEP, a selective mGluR5 antagonist, in methamphetamine-induced dopaminergic neurotoxicity is associated with a decrease in dopamine outflow and inhibition of hyperthermia in rats. Gołembiowska, K., Konieczny, J., Wolfarth, S., Ossowska, K. Neuropharmacology (2003) [Pubmed]
  15. The role of metabotropic glutamate receptors in regulation of striatal proenkephalin expression: implications for the therapy of Parkinson's disease. Wardas, J., Pietraszek, M., Wolfarth, S., Ossowska, K. Neuroscience (2003) [Pubmed]
  16. Role of synaptic metabotropic glutamate receptors in epileptiform discharges in hippocampal slices. Lee, A.C., Wong, R.K., Chuang, S.C., Shin, H.S., Bianchi, R. J. Neurophysiol. (2002) [Pubmed]
  17. mGluR1, but not mGluR5, mediates depolarization of spinal cord neurons by blocking a leak current. Kettunen, P., Hess, D., El Manira, A. J. Neurophysiol. (2003) [Pubmed]
  18. Chronic exposure to ammonia alters the modulation of phosphorylation of microtubule-associated protein 2 by metabotropic glutamate receptors 1 and 5 in cerebellar neurons in culture. Llansola, M., Erceg, S., Felipo, V. Neuroscience (2005) [Pubmed]
  19. Endogenous activation of mGlu5 metabotropic glutamate receptors supports self-renewal of cultured mouse embryonic stem cells. Cappuccio, I., Spinsanti, P., Porcellini, A., Desiderati, F., De Vita, T., Storto, M., Capobianco, L., Battaglia, G., Nicoletti, F., Melchiorri, D. Neuropharmacology (2005) [Pubmed]
  20. Synthesis and structure-activity relationships of 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine analogues as potent, noncompetitive metabotropic glutamate receptor subtype 5 antagonists; search for cocaine medications. Iso, Y., Grajkowska, E., Wroblewski, J.T., Davis, J., Goeders, N.E., Johnson, K.M., Sanker, S., Roth, B.L., Tueckmantel, W., Kozikowski, A.P. J. Med. Chem. (2006) [Pubmed]
  21. mGlu(5) receptors are involved in the discriminative stimulus effects of self-administered ethanol in rats. Besheer, J., Stevenson, R.A., Hodge, C.W. Eur. J. Pharmacol. (2006) [Pubmed]
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