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™.
Sold with the permission of Eli Lilly and Company
|Storage||Desiccate at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 209.2. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||4.78 mL||23.9 mL||47.8 mL|
|5 mM||0.96 mL||4.78 mL||9.56 mL|
|10 mM||0.48 mL||2.39 mL||4.78 mL|
|50 mM||0.1 mL||0.48 mL||0.96 mL|
References are publications that support the biological activity of the product.
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 recept 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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Keywords: LY 367385, LY 367385 supplier, Selective, mGlu1a, mGluR1a, antagonist, Group, I, Receptors, Glutamate, Metabotropic, LY367385, (Metabotropic), 1237, Tocris Bioscience
42 Citations for LY 367385
Citations are publications that use Tocris products. Selected citations for LY 367385 include:
Thalman et al (2018) Synaptic phospholipids as a new target for cortical hyperexcitability and E/I balance in psychiatric disorders. Mol Psychiatry 23 1699 PMID: 29743582
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
Dornier (2017) Glutaminolysis drives membrane trafficking to promote invasiveness of breast cancer cells. Nat Commun 8 2255 PMID: 29269878
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
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
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
Dominguez et al (2013) Membrane-initiated estradiol signaling in immortalized hypothalamic N-38 neurons. J Neurosci 78 607 PMID: 23296142
Boulware et al (2013) The memory-enhancing effects of hippocampal estrogen receptor activation involve metabotropic glutamate receptor signaling. Mol Pharmacol 33 15184 PMID: 24048848
Fanselow et al (2008) Selective, state-dependent activation of somatostatin-expressing inhibitory interneurons in mouse neocortex. J Neurophysiol 100 2640 PMID: 18799598
Zhang et al (2008) The tyrosine phosphatase STEP mediates AMPA receptor endocytosis after metabotropic glutamate receptor stimulation. J Neurosci 28 10561 PMID: 18923032
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
Bozdagi et al (2012) Haploinsufficiency of Cyfip1 produces fragile X-like phenotypes in mice. Steroids 7 e42422 PMID: 22900020
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
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
Sossa et al (2007) AMPAR exocytosis through NO modulation of PICK1. J Neurosci 53 92 PMID: 17555774
Zhao et al (2015) Extracellular glutamate exposure facilitates group I mGluR-mediated epileptogenesis in the hippocampus. J Neurophysiol 35 308 PMID: 25568123
Vasuta et al (2015) Metaplastic Regulation of CA1 Schaffer Collateral Pathway Plasticity by Hebbian MGluR1a-Mediated Plasticity at Excitatory Synapses onto Somatostatin-Expressing Interneurons(1,2,3). J Neurosci 2 PMID: 26464997
Cramer et al (2015) Abnormal excitability and episodic low-frequency oscillations in the cerebral cortex of the tottering mouse. Proc Natl Acad Sci U S A 35 5664 PMID: 25855180
Ramiro-Cortés (2013) Long lasting protein synthesis- and activity-dependent spine shrinkage and elimination after synaptic depression. PLoS One 8 e71155 PMID: 23951097
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
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
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
Clem and Huganir (2013) Norepinephrine enhances a discrete form of long-term depression during fear memory storage. J Neurosci 33 11825 PMID: 23864672
Zhang and Lisman (2012) Activity-dependent regulation of synaptic strength by PSD-95 in CA1 neurons. Eneuro 107 1058 PMID: 22114157
Peterfi et al (2012) Endocannabinoid-mediated long-term depression of afferent excitatory synapses in hippocampal pyramidal cells and GABAergic interneurons. J Neurosci 32 14448 PMID: 23055515
Reissner et al (2010) A novel postsynaptic mechanism for heterosynaptic sharing of short-term plasticity. J Neurosci 30 8797 PMID: 20592201
Jung et al (2005) Stimulation of endocannabinoid formation in brain slice cultures through activation of group I metabotropic glutamate receptors. Br J Pharmacol 68 1196 PMID: 16051747
Gallagher et al (2004) Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1. J Neurosci 24 4859 PMID: 15152046
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
Krishnan et al (2011) Dopamine-induced plasticity, phospholipase D (PLD) activity and cocaine-cue behavior depend on PLD-linked metabotropic glutamate receptors in amygdala. PLoS One 6 e25639 PMID: 21980514
Castro and Urban (2009) Subthreshold glutamate release from mitral cell dendrites. J Neurosci 29 7023 PMID: 19474329
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
Wu et al (2004) Group I metabotropic glutamate receptor activation produces a direct excitation of identified septohippocampal cholinergic neurons. J Neurophysiol 92 1216 PMID: 15044519
Nishi et al (2003) Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling. PLoS One 100 1322 PMID: 12538871
Galván et al (2015) Synapse-specific compartmentalization of signaling cascades for LTP induction in CA3 interneurons. Neuroscience 290 332 PMID: 25637803
Hullinger et al (2015) 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. Neurobiol Learn Mem 125 126 PMID: 26341144
Bondar et al (2009) Estradiol-induced estrogen receptor-α trafficking. J Neurosci 29 15323 PMID: 19955385
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Huntington's Disease Poster
Huntington's disease (HD) is a monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the MSN intracellular signaling pathways implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.