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Chemical Compound Review

Tocris-1237     4-[(S)-amino-carboxy-methyl]- 3-methyl...

Synonyms: AC1NSKBK, CHEMBL94631, SureCN661700, CHEBI:252690, LY-367385, ...
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Disease relevance of Tocris-1237


Psychiatry related information on Tocris-1237


High impact information on Tocris-1237

  • Three group I mGluR antagonists CPCCOEt, LY367385 and BAY36-7620, were analyzed for their effect on cell surface expression of metabotropic glutamate receptor 1a and 1b [5].
  • Application of DHPG (5-100 microM) reduced the field EPSP, and this effect could be reversed by the mGluR1 antagonist LY367385 (200 microM), but not by the mGluR5 antagonist MPEP (5 microM) [6].
  • High-frequency ON stimulation in the presence of NBQX and D-APV also evoked a slow, nearly 2-Hz oscillation of MC membrane potential that was abolished by the mGluR1 antagonist LY367385 (50 microM) [7].
  • The mGluR1 antagonists LY367385 (10 microM, 72 h) markedly decreased the number of TOAD-64 positive cells and mGluR5 antagonist MPEP (1 microM, 72 h) had no effect [8].
  • Injections of LY367385 at all concentrations under investigation (4-32 nmol in a 5-microL injection volume) did not affect basal synaptic transmission [4].

Chemical compound and disease context of Tocris-1237

  • Baclofen, an agonist of GABA(B) receptors and LY367385, an antagonist of mGluR(1a) receptors, given alone or jointly, reduced the immobility time in the forced swim test but only their separate administration enhanced motility in group of rats without hypoxia [3].

Biological context of Tocris-1237

  • The first part of this synaptic response and the agonist-induced depolarization of membrane potential were depressed by the novel group I receptor antagonists LY367366 and LY367385, which are active at mGlu1 receptors [9].
  • Since activation of PLC is thought to be associated with cell proliferation, we investigated whether group I mGluR agonist DHPG or subtype antagonists LY367385 and MPEP have an effect on dentate granule cells expressing immature neuronal marker TOAD-64 [8].
  • Further antagonist actions were also demonstrated in a model of (RS)-DHPG-induced PI hydrolysis in vivo such that LY367385 and the active cis isomer of LY393053 produced dose-dependent inhibition of PI responses in both cerebellum and hippocampus [10].

Anatomical context of Tocris-1237

  • Post-treatment with the group I mGlu receptor antagonists LY367385 and AIDA allowed significant recovery of the paw withdrawal latencies after the onset of the knee joint inflammation [11].
  • In addition, the increase in the frequency of spontaneous IPSCs (sIPSCs) caused by the DHPG-induced depolarization of inhibitory interneurons also was blocked by LY367385, as was the DHPG-induced inhibition of transmission at the Schaffer collateral-->CA1 synapse [12].

Associations of Tocris-1237 with other chemical compounds

  • In the presence of the competitive mGluR1 antagonist LY367385, the NMDA responses were potentiated in the presence of CHPG, whereas the CHPG-induced enhancement was not observed in slices treated with the non-competitive mGluR5 antagonist 2-methyl-6-(phenylethynyl)-pyridine [13].
  • However, preincubation with both MPEP and the mGluR1 antagonist LY367385 completely prevented the DHPG-induced changes [14].
  • The DHPG-evoked inward current was unaffected by the mGluR1 antagonist (S)-(+)-alpha-amino-4-carboxy-2-methylbenzeneacetic acid (LY367385), was blocked by the group I/II mGluR antagonist (alphaS)-alpha-amino-alpha-[(1S,2S)-2-carboxycyclopropyl]-9H-xanthine-9-propanoic acid (LY341495), and was absent in GCs from mGluR5 knockout mice [15].
  • In addition, MPEP (a selective mGluR5 antagonist) partially reduced ouabain, endobain E and glutamate responses and the selective mGluR1 antagonist LY367385 showed no activity at all [16].

Gene context of Tocris-1237

  • This was strongly reduced by the broad-spectrum antagonist (+)-alpha-methyl-4-carboxyphenylglycine (MCPG, 1 mm, approximately 95% reduction), by the mGluR1 antagonist LY367385 (100 microm, approximately 80% reduction) but not by the mGluR5 antagonist 6-methyl-2-(phenylethynyl)-pyridine (MPEP, 1-100 microm) [17].
  • In normal awake conditions, the spontaneous firing rates of neurons in the pallidal complex were increased by DHPG, a selective agonist of group I mGluRs, whereas they were decreased by AIDA, a selective antagonist of group I mGluRs, or LY367385, a selective antagonist of mGluR1 [18].


  1. Selective blockade of type-1 metabotropic glutamate receptors induces neuroprotection by enhancing gabaergic transmission. Battaglia, G., Bruno, V., Pisani, A., Centonze, D., Catania, M.V., Calabresi, P., Nicoletti, F. Mol. Cell. Neurosci. (2001) [Pubmed]
  2. Neuroprotective actions of novel and potent ligands of group I and group II metabotropic glutamate receptors. Kingston, A.E., O'Neill, M.J., Bond, A., Bruno, V., Battaglia, G., Nicoletti, F., Harris, J.R., Clark, B.P., Monn, J.A., Lodge, D., Schoepp, D.D. Ann. N. Y. Acad. Sci. (1999) [Pubmed]
  3. Antidepressant-like effects of baclofen and LY367385 in the forced swim test in rats. Car, H., Wi??niewskao, R.J. Pharmacological reports : PR (2006) [Pubmed]
  4. Pharmacological antagonism of metabotropic glutamate receptor 1 regulates long-term potentiation and spatial reference memory in the dentate gyrus of freely moving rats via N-methyl-D-aspartate and metabotropic glutamate receptor-dependent mechanisms. Naie, K., Manahan-Vaughan, D. Eur. J. Neurosci. (2005) [Pubmed]
  5. Agonist-independent internalization of metabotropic glutamate receptor 1a is arrestin- and clathrin-dependent and is suppressed by receptor inverse agonists. Pula, G., Mundell, S.J., Roberts, P.J., Kelly, E. J. Neurochem. (2004) [Pubmed]
  6. Group I metabotropic glutamate receptors (mGluRs) modulate visual responses in the superficial superior colliculus of the rat. Cirone, J., Pothecary, C.A., Turner, J.P., Salt, T.E. J. Physiol. (Lond.) (2002) [Pubmed]
  7. Olfactory nerve stimulation-evoked mGluR1 slow potentials, oscillations, and calcium signaling in mouse olfactory bulb mitral cells. Yuan, Q., Knöpfel, T. J. Neurophysiol. (2006) [Pubmed]
  8. Group I metabotropic glutamate receptors reduce excitotoxic injury and may facilitate neurogenesis. Baskys, A., Bayazitov, I., Fang, L., Blaabjerg, M., Poulsen, F.R., Zimmer, J. Neuropharmacology (2005) [Pubmed]
  9. Synaptic activation of the group I metabotropic glutamate receptor mGlu1 on the thalamocortical neurons of the rat dorsal lateral geniculate nucleus in vitro. Turner, J.P., Salt, T.E. Neuroscience (2000) [Pubmed]
  10. Inhibition of group I metabotropic glutamate receptor responses in vivo in rats by a new generation of carboxyphenylglycine-like amino acid antagonists. Kingston, A.E., Griffey, K., Johnson, M.P., Chamberlain, M.J., Kelly, G., Tomlinson, R., Wright, R.A., Johnson, B.G., Schoepp, D.D., Harris, J.R., Clark, B.P., Baker, R.S., Tizzano, J.T. Neurosci. Lett. (2002) [Pubmed]
  11. Group I metabotropic glutamate receptor antagonists block secondary thermal hyperalgesia in rats with knee joint inflammation. Zhang, L., Lu, Y., Chen, Y., Westlund, K.N. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  12. Metabotropic glutamate receptors 1 and 5 differentially regulate CA1 pyramidal cell function. Mannaioni, G., Marino, M.J., Valenti, O., Traynelis, S.F., Conn, P.J. J. Neurosci. (2001) [Pubmed]
  13. Metabotropic glutamate receptor 5 mediates the potentiation of N-methyl-D-aspartate responses in medium spiny striatal neurons. Pisani, A., Gubellini, P., Bonsi, P., Conquet, F., Picconi, B., Centonze, D., Bernardi, G., Calabresi, P. Neuroscience (2001) [Pubmed]
  14. Group I mGluRs increase excitability of hippocampal CA1 pyramidal neurons by a PLC-independent mechanism. Ireland, D.R., Abraham, W.C. J. Neurophysiol. (2002) [Pubmed]
  15. Metabotropic glutamate receptors in the main olfactory bulb drive granule cell-mediated inhibition. Heinbockel, T., Laaris, N., Ennis, M. J. Neurophysiol. (2007) [Pubmed]
  16. Metabotropic glutamate receptor involvement in phosphoinositide hydrolysis stimulation by an endogenous Na(+), K(+)-ATPase inhibitor and ouabain in neonatal rat brain. Calviño, M.A., Peña, C., Rodríguez de Lores Arnaiz, G. Brain Res. Dev. Brain Res. (2002) [Pubmed]
  17. Presynaptic group I metabotropic glutamate receptors modulate synaptic transmission in the rat superior colliculus via 4-AP sensitive K(+) channels. White, A.M., Kylänpää, R.A., Christie, L.A., McIntosh, S.J., Irving, A.J., Platt, B. Br. J. Pharmacol. (2003) [Pubmed]
  18. Down-regulation of metabotropic glutamate receptor 1alpha in globus pallidus and substantia nigra of parkinsonian monkeys. Kaneda, K., Tachibana, Y., Imanishi, M., Kita, H., Shigemoto, R., Nambu, A., Takada, M. Eur. J. Neurosci. (2005) [Pubmed]
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