LY 367385

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1237/10
1237/50
LY 367385 | CAS No. 198419-91-9 | Group I mGluR Antagonists
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Description: Selective mGlu1a antagonist

Chemical Name: (S)-(+)-α-Amino-4-carboxy-2-methylbenzeneacetic acid

Product Details
Citations (47)
Supplemental Products
Reviews (1)

Biological Activity

A selective mGlu1a receptor antagonist, with an IC50 value of 8.8 μM for blockade of quisqualate-induced phosphoinositide hydrolysis vs. > 100 μM for mGlu5a, and negligible action on group II and III receptors. Also available as part of the Group I mGlu Receptor Tocriset™.

Technical Data

Formula:
C10H11NO4
Solubility:
Soluble to 100 mM in 1.1eq. NaOH
Storage:
Store the unopened product at room temperature. Do not use past expiration date.
CAS No:
198419-91-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of Eli Lilly and Company

Background References

  1. Olanzapine: preclinical and clinical profiles of a novel antipsychotic agent.
    Tollefson and Taylor
    CNS Drug Reviews, 2000;6:303
  2. Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4 carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum antagonist with equal affinity for mGlu1a and mGlu5 recept
    Bruno et al.
    Neuropharmacology, 1999;38:199
  3. Anticonvulsant actions of LY 367385 ((+)-methyl-4-carboxyphenylglycine), and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid).
    Chapman et al.
    Eur.J.Pharmacol., 1999;368:17
  4. Reduction of sensory and metabotropic glutamate receptor responses in the thalamus by the novel metabotropic glutamate receptor-1-selective antagonist S-2-methyl-4-carboxy-phenylglycine.
    Salt and Turner
    Neuroscience, 1998;85:655
  5. (+)-2-Methyl-4-carboxyphenylglycine (LY 367385) selectively antagonises metabotropic glutamate mGluR1 receptors.
    Clark et al.
    Bioorg.Med.Chem.Lett., 1997;7:2777

Product Datasheets

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Citations for LY 367385

The citations listed below are publications that use Tocris products. Selected citations for LY 367385 include:

47 Citations: Showing 1 - 10

  1. Activation of Astrocytic μ-Opioid Receptor Causes Conditioned Place Preference.
    Authors: Nam Et al.
    Cell Rep  2019;28:1154
  2. A group I metabotropic glutamate receptor controls synaptic gain between rods and rod bipolar cells in the mouse retina.
    Authors: Hellmer Et al.
    Physiol Rep  2018;6:e13885
  3. Synaptic phospholipids as a new target for cortical hyperexcitability and E/I balance in psychiatric disorders.
    Authors: Thalman Et al.
    Mol Psychiatry  2018;23(8):1699
  4. Astrocytic Activation Generates De Novo Neuronal Potentiation and Memory Enhancement.
    Authors: Adamsky Et al.
    Cell  2018;174:59
  5. Presynaptic mGlu1 Receptors Control GABAB Receptors in an Antagonist-Like Manner in Mouse Cortical GABAergic and Glutamatergic Nerve Endings.
    Authors: Vergassola Et al.
    Front Mol Neurosci  2018;11:324
  6. LTP at Hilar Mossy Cell-Dentate Granule Cell Synapses Modulates Dentate Gyrus Output by Increasing Excitation/Inhibition Balance.
    Authors: Hashimotodani Et al.
    Neuron  2017;95:928
  7. Glutaminolysis drives membrane trafficking to promote invasiveness of breast cancer cells.
    Authors: Dornier
    Nat Commun  2017;8(1):2255
  8. Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse.
    Authors: Cramer Et al.
    Proc Natl Acad Sci U S A  2015;35:5664
  9. Homer protein-metabotropic glutamate receptor binding regulates endocannabinoid signaling and affects hyperexcitability in a mouse model of fragile X syndrome.
    Authors: Tang and Alger
    J Neurosci  2015;35:3938
  10. Extracellular glutamate exposure facilitates group I mGluR-mediated epileptogenesis in the hippocampus.
    Authors: Zhao Et al.
    J Neurophysiol  2015;35:308
  11. Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons.
    Authors: Galván Et al.
    Neuroscience  2015;290:332
  12. Metaplastic Regulation of CA1 Schaffer Collateral Pathway Plasticity by Hebbian MGluR1a-Mediated Plasticity at Excitatory Synapses onto Somatostatin-Expressing Interneurons(1,2,3).
    Authors: Vasuta Et al.
    J Neurosci  2015;2
  13. Environmental enrichment improves learning and memory and long-term potentiation in young adult rats through a mechanism requiring mGluR5 signaling and sustained activation of p70s6k.
    Authors: Hullinger Et al.
    Neurobiol Learn Mem  2015;125:126
  14. mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways.
    Authors: Kubota Et al.
    PLoS One  2014;9:e106316
  15. Mutant β-III spectrin causes mGluR1α mislocalization and functional deficits in a mouse model of spinocerebellar ataxia type 5.
    Authors: Armbrust Et al.
    J Neurosci  2014;34:9891
  16. Long lasting protein synthesis- and activity-dependent spine shrinkage and elimination after synaptic depression.
    Authors: Ramiro-Cortés
    PLoS One  2013;8:e71155
  17. Membrane-initiated OE signaling in immortalized hypothalamic N-38 neurons.
    Authors: Dominguez Et al.
    J Neurosci  2013;78:607
  18. The memory-enhancing effects of hippocampal estrogen receptor activation involve metabotropic glutamate receptor signaling.
    Authors: Boulware Et al.
    Mol Pharmacol  2013;33:15184
  19. NE enhances a discrete form of long-term depression during fear memory storage.
    Authors: Clem and Huganir
    J Neurosci  2013;33:11825
  20. Optogenetic stimulation of the corticothalamic pathway affects relay cells and GABAergic neurons differently in the mouse visual thalamus.
    Authors: Jurgens Et al.
    PLoS One  2012;7:e45717
  21. Haploinsufficiency of Cyfip1 produces fragile X-like phenotypes in mice.
    Authors: Bozdagi Et al.
    Steroids  2012;7:e42422
  22. Endocannabinoid-mediated long-term depression of afferent excitatory synapses in hippocampal pyramidal cells and GABAergic interneurons.
    Authors: Peterfi Et al.
    J Neurosci  2012;32:14448
  23. Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses.
    Authors: Caiati Et al.
    Sci Rep  2012;2:285
  24. Activity-dependent regulation of synaptic strength by PSD-95 in CA1 neurons.
    Authors: Zhang and Lisman
    Eneuro  2012;107:1058
  25. DA-induced plasticity, phospholipase D (PLD) activity and cocaine-cue behavior depend on PLD-linked metabotropic glutamate receptors in amygdala.
    Authors: Krishnan Et al.
    PLoS One  2011;6:e25639
  26. Altered neocortical rhythmic activity states in Fmr1 KO mice are due to enhanced mGluR5 signaling and involve changes in excitatory circuitry.
    Authors: Hays Et al.
    J Neurosci  2011;31:14223
  27. A novel postsynaptic mechanism for heterosynaptic sharing of short-term plasticity.
    Authors: Reissner Et al.
    J Neurosci  2010;30:8797
  28. Modulator property of the intrinsic cortical projection from layer 6 to layer 4.
    Authors: Lee and Sherman
    Front Syst Neurosci  2009;3:3
  29. Subthreshold glutamate release from mitral cell dendrites.
    Authors: Castro and Urban
    J Neurosci  2009;29:7023
  30. OE-induced estrogen receptor-α trafficking.
    Authors: Bondar Et al.
    J Neurosci  2009;29:15323
  31. Differential distribution of endoplasmic reticulum controls metabotropic signaling and plasticity at hippocampal synapses.
    Authors: Holbro Et al.
    Proc Natl Acad Sci U S A  2009;106:15055
  32. The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation.
    Authors: Zhang Et al.
    J Neurosci  2008;28:10561
  33. Metabotropic glutamate receptor 1 (mGluR1) and 5 (mGluR5) regulate late phases of LTP and LTD in the hippocampal CA1 region in vitro.
    Authors: Neyman and Manahan-Vaughan
    Eur J Neurosci  2008;27:1345
  34. Selective, state-dependent activation of somatostatin-expressing inhibitory interneurons in mouse neocortex.
    Authors: Fanselow Et al.
    J Neurophysiol  2008;100:2640
  35. AMPAR exocytosis through NO modulation of PICK1.
    Authors: Sossa Et al.
    J Neurosci  2007;53:92
  36. Calpain-mediated mGluR1alpha truncation: a key step in excitotoxicity.
    Authors: Xu Et al.
    Neuron  2007;53:399
  37. Loss of metabotropic glutamate receptor-dependent long-term depression via downregulation of mGluR5 after status epilepticus.
    Authors: Kirschstein Et al.
    J Neurosci  2007;27:7696
  38. Dysregulated metabotropic glutamate receptor-dependent translation of AMPA receptor and postsynaptic density-95 mRNAs at synapses in a mouse model of fragile X syndrome.
    Authors: Muddashetty Et al.
    J Neurosci  2007;27:5338
  39. Fragile X mental retardation protein deficiency leads to excessive mGluR5-dependent internalization of AMPA receptors.
    Authors: Nakamoto Et al.
    Proc Natl Acad Sci U S A  2007;104:15537
  40. Visual experience regulates metabotropic glutamate receptor-mediated plasticity of AMPA receptor synaptic transmission by homer1a induction.
    Authors: Keuren-Jensen and Cline
    J Neurosci  2006;26:7575
  41. Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptors.
    Authors: Jung Et al.
    Br J Pharmacol  2005;68:1196
  42. Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons.
    Authors: Calò Et al.
    J Neurosci  2005;25:2245
  43. Group I metabotropic glutamate receptor activation produces a direct excitation of identified septohippocampal cholinergic neurons.
    Authors: Wu Et al.
    J Neurophysiol  2004;92:1216
  44. Endocannabinoid-mediated metaplasticity in the hippocampus.
    Authors: Chevaleyre and Castillo
    Neuron  2004;43:871
  45. Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1.
    Authors: Gallagher Et al.
    J Neurosci  2004;24:4859
  46. Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons.
    Authors: Huang Et al.
    J Neurosci  2004;24:4551
  47. Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling.
    Authors: Nishi Et al.
    PLoS One  2003;100:1322

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Used in inhibitor cocktail
By Anonymous on 12/03/2019
Species: Rat

Retinal dissections were performed in HEPES-buffered extracellular solution containing inhibitor cocktail containing 100 umol/L LY 367385

PMID: 30338673

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