Cat. No. 1237
Chemical Name: (S)-(+)-α-Amino-4-carboxy-2-methylbe
Biological ActivityA 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™.
Licensing InformationSold with the permission of Eli Lilly and Company
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Bruno et al (1999) 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 receptors. Neuropharmacology 38 199. PMID: 10218860.
Chapman et al (1999) Anticonvulsant actions of LY 367385 ((+)-methyl-4-carboxyphenylglycine), and AIDA ((RS)-1-aminoindan-1,5-dicarboxylic acid). Eur.J.Pharmacol. 368 17. PMID: 10096765.
Salt and Turner (1998) 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. Neuroscience 85 655. PMID: 9639261.
Clark et al (1997) (+)-2-Methyl-4-carboxyphenylglycine (LY 367385) selectively antagonises metabotropic glutamate mGluR1 receptors. Bioorg.Med.Chem.Lett. 7 2777.
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Citations are publications that use Tocris products. Selected citations for LY 367385 include:
Tang and Alger (2015) Homer protein-metabotropic glutamate receptor binding regulates endocannabinoid signaling and affects hyperexcitability in a mouse model of fragile X syndrome. J Neurosci 35 3938. PMID: 25740522.
Armbrust et al (2014) Mutant β-III spectrin causes mGluR1α mislocalization and functional deficits in a mouse model of spinocerebellar ataxia type 5. J Neurosci 34 9891. PMID: 25057192.
Kubota et al (2014) mGluR1-mediated excitation of cerebellar GABAergic interneurons requires both G protein-dependent and Src-ERK1/2-dependent signaling pathways. PLoS One 9 e106316. PMID: 25181481.
Caiati et al (2012) Developmental regulation of CB1-mediated spike-time dependent depression at immature mossy fiber-CA3 synapses. Sci Rep 2 285. PMID: 22368777.
Jurgens et al (2012) Optogenetic stimulation of the corticothalamic pathway affects relay cells and GABAergic neurons differently in the mouse visual thalamus. PLoS One 7 e45717. PMID: 23029198.
Hays et al (2011) Altered neocortical rhythmic activity states in Fmr1 KO mice are due to enhanced mGluR5 signaling and involve changes in excitatory circuitry. J Neurosci 31 14223. PMID: 21976507.
Holbro et al (2009) Differential distribution of endoplasmic reticulum controls metabotropic signaling and plasticity at hippocampal synapses. Proc Natl Acad Sci U S A 106 15055. PMID: 19706463.
Lee and Sherman (2009) Modulator property of the intrinsic cortical projection from layer 6 to layer 4. Front Syst Neurosci 3 3. PMID: 19277215.
Fanselow et al (2008) Selective, state-dependent activation of somatostatin-expressing inhibitory interneurons in mouse neocortex. J Neurophysiol 100 2640. PMID: 18799598.
Neyman and Manahan-Vaughan (2008) Metabotropic glutamate receptor 1 (mGluR1) and 5 (mGluR5) regulate late phases of LTP and LTD in the hippocampal CA1 region in vitro. Eur J Neurosci 27 1345. PMID: 18364018.
Zhang et al (2008) The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation. J Neurosci 28 10561. PMID: 18923032.
Kirschstein et al (2007) Loss of metabotropic glutamate receptor-dependent long-term depression via downregulation of mGluR5 after status epilepticus. J Neurosci 27 7696. PMID: 17634364.
Muddashetty et al (2007) Dysregulated metabotropic glutamate receptor-dependent translation of AMPA receptor and postsynaptic density-95 mRNAs at synapses in a mouse model of fragile X syndrome. J Neurosci 27 5338. PMID: 17507556.
Nakamoto et al (2007) Fragile X mental retardation protein deficiency leads to excessive mGluR5-dependent internalization of AMPA receptors. Proc Natl Acad Sci U S A 104 15537. PMID: 17881561.
Xu et al (2007) Calpain-mediated mGluR1alpha truncation: a key step in excitotoxicity. Neuron 53 399. PMID: 17270736.
Keuren-Jensen and Cline (2006) Visual experience regulates metabotropic glutamate receptor-mediated plasticity of AMPA receptor synaptic transmission by homer1a induction. J Neurosci 26 7575. PMID: 16855085.
Calò et al (2005) Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons. J Neurosci 25 2245. PMID: 15745950.
Chevaleyre and Castillo (2004) Endocannabinoid-mediated metaplasticity in the hippocampus. Neuron 43 871. PMID: 15363397.
Huang et al (2004) Astrocyte glutamate transporters regulate metabotropic glutamate receptor-mediated excitation of hippocampal interneurons. J Neurosci 24 4551. PMID: 15140926.
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Keywords: LY 367385, supplier, Selective, mGlu1a, mGluR1a, antagonist, Group, I, Receptors, Glutamate, Metabotropic, LY367385, Tocris Bioscience, Glutamate (Metabotropic) Group I Receptor Antagonist products
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