LY 341495

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Cat.No. 1209 - LY 341495 | C20H19NO5 | CAS No. 201943-63-7
Description: Highly potent and selective group II mGlu antagonist
Chemical Name: (2S)-2-Amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xanth-9-yl) propanoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (62)
Reviews
Literature

Biological Activity

Highly potent and selective group II metabotropic glutamate receptor antagonist (Ki/IC50 values are 2.3, 1.3, 173, 990, 6800, 8200 and 22000 nM for human mGlu2, mGlu3, mGlu8, mGlu7a, mGlu1a, mGlu5a and mGlu4a receptors respectively). Readily brain penetrant and active in vivo. Disodium salt (Cat. No. 4062) also available. Also available as part of the Group II mGlu Receptor Tocriset™, Group III mGlu Receptor Tocriset™ and Mixed mGlu Receptor Tocriset™.

Licensing Information

Sold with the permission of Eli Lilly and Company

Technical Data

M. Wt 353.37
Formula C20H19NO5
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 201943-63-7
PubChem ID 9819927
InChI Key VLZBRVJVCCNPRJ-KPHUOKFYSA-N
Smiles [H][C@]4([C@@H]([C@](O)=O)C4)[C@](N)(C(O)=O)CC2C3=C(C=CC=C3)OC1=CC=CC=C12

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 3.61 10 with gentle warming
1.2eq. NaOH 35.34 100

Preparing Stock Solutions

The following data is based on the product molecular weight 353.37. 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 2.83 mL 14.15 mL 28.3 mL
5 mM 0.57 mL 2.83 mL 5.66 mL
10 mM 0.28 mL 1.41 mL 2.83 mL
50 mM 0.06 mL 0.28 mL 0.57 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Fitzjohn et al (1998) The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology 37 1445 PMID: 9886667

Johnson et al (1999) [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells. Neuropharmacology 38 1519 PMID: 10530814

Kingston et al (1998) LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology 37 1 PMID: 9680254

Ornstein et al (1998) 2-Substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl) glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioav J.Med.Chem. 41 358 PMID: 9464367


If you know of a relevant reference for LY 341495, please let us know.

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Keywords: LY 341495, LY 341495 supplier, Group, II/III, antagonists, potent, selective, group, II, mGlur, III, Receptors, mGlu4, mGlu6, mGlu7, mGlu8, mGlu4R, mGlu6R, mGlu7R, mGlu8R, Glutamate, Metabotropic, mGlu2, mGlu3, mGluR2, mGluR3, LY341495, (Metabotropic), 1209, Tocris Bioscience

62 Citations for LY 341495

Citations are publications that use Tocris products. Selected citations for LY 341495 include:

Taman and Ribeiro (2011) Characterization of a truncated metabotropic glutamate receptor in a primitive metazoan, the parasitic flatworm Schistosoma mansoni. PLoS One 6 e27119 PMID: 22069494

Biou et al (2008) Endocytosis and recycling of AMPA receptors lacking GluR2/3. PLoS One 105 1038 PMID: 18195348

Baker et al (2008) Contribution of cystine-glutamate antiporters to the psychotomimetic effects of phencyclidine. J Neurosci 33 1760 PMID: 17728701

Olszewski et al (2008) Phencyclidine and dizocilpine induced behaviors reduced by N-acetylaspartylglutamate peptidase inhibition via metabotropic glutamate receptors. Biol Psychiatry 63 86 PMID: 17597589

Johnson (2017) Metabotropic glutamate receptor 2 inhibits thalamically-driven glutamate and dopamine release in the dorsal striatum Neuropharmacology 117 114 PMID: 28159646

Dornier (2017) Glutaminolysis drives membrane trafficking to promote invasiveness of breast cancer cells. Nat Commun 8 2255 PMID: 29269878

Grimes et al (2014) Cross-synaptic synchrony and transmission of signal and noise across the mouse retina. Elife 3 e03892 PMID: 25180102

Miyamoto et al (2014) Overexpression of Shati/Nat8l, an N-acetyltransferase, in the nucleus accumbens attenuates the response to methamphetamine via activation of group II mGluRs in mice. Int J Neuropsychopharmacol 17 1283 PMID: 24559655

Wang et al (2013) Group II metabotropic glutamate receptor agonist LY379268 regulates AMPA receptor trafficking in prefrontal cortical neurons. Neurosci Lett 8 e61787 PMID: 23593498

Kaushal and Schlichter (2008) Mechanisms of microglia-mediated neurotoxicity in a new model of the stroke penumbra. Glia 28 2221 PMID: 18305255

Russo et al (2008) Dynamic metabotropic control of intrinsic firing in cerebellar unipolar brush cells. J Neurophysiol 100 3351 PMID: 18945818

Sheffler and Conn (2008) Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology 55 419 PMID: 18625258

Huang et al (2008) Roles of endocannabinoids in heterosynaptic long-term depression of excitatory synaptic transmission in visual cortex of young mice. J Neurosci 28 7074 PMID: 18614676

Scholler (2017) HTS-compatible FRET-based conformational sensors clarify membrane receptor activation. Nat Chem Biol 13 372 PMID: 28135236

Scholler (2017) Allosteric nanobodies uncover a role of hippocampal mGlu2 receptor homodimers in contextual fear consolidation. Nat Commun 8 1967 PMID: 29213077

Marrocco et al (2012) Anxiety-like behavior of prenatally stressed rats is associated with a selective reduction of glutamate release in the ventral hippocampus. Acta Crystallogr Sect F Struct Biol Cryst Commun 32 17143 PMID: 23197707

Peachey et al (2012) Depolarizing bipolar cell dysfunction due to a Trpm1 point mutation. Brain Res 108 2442 PMID: 22896717

Johnson et al (2011) Activation of group II metabotropic glutamate receptors induces long-term depression of excitatory synaptic transmission in the substantia nigra pars reticulata. Addict Biol 504 102 PMID: 21945652

Pearring et al (2011) A role for nyctalopin, a small leucine-rich repeat protein, in localizing the TRP melastatin 1 channel to retinal depolarizing bipolar cell dendrites. Proc Natl Acad Sci U S A 31 10060 PMID: 21734298

Ster et al (2011) Enhancement of CA3 hippocampal network activity by activation of group II metabotropic glutamate receptors. J Endocrinol 108 9993 PMID: 21628565

Duguid et al (2007) Somatodendritic release of glutamate regulates synaptic inhibition in cerebellar Purkinje cells via autocrine mGluR1 activation. J Neurosci 27 12464 PMID: 18003824

Brager and Johnston (2007) Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons. J Neurosci 27 13926 PMID: 18094230

Woo et al (2007) Neuregulin-1 enhances depolarization-induced GABA release. Neuron 54 599 PMID: 17521572

Gee et al (2014) Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior. J Biol Chem 289 10975 PMID: 24596089

Kim et al (2010) Group II metabotropic glutamate receptor stimulation triggers production and release of Alzheimer's amyloid(β)42 from isolated intact nerve terminals. Proc Natl Acad Sci U S A 30 3870 PMID: 20237257

Rosa et al (2015) Neuron-glia signaling in developing retina mediated by neurotransmitter spillover. J Neurosci 4 PMID: 26274565

Garthwaite et al (2015) Nitric oxide targets oligodendrocytes and promotes their morphological differentiation. Mol Pain 63 383 PMID: 25327839

Truini et al (2015) N-acetyl-cysteine, a drug that enhances the endogenous activation of group-II metabotropic glutamate receptors, inhibits nociceptive transmission in humans. J Neurosci 11 14 PMID: 25889381

Choi et al (2015) PDE-4 inhibition rescues aberrant synaptic plasticity in Drosophila and mouse models of fragile X syndrome. Psychopharmacology (Berl) 35 396 PMID: 25568131

Carbonaro et al (2015) The role of 5-HT2A, 5-HT 2C and mGlu2 receptors in the behavioral effects of tryptamine hallucinogens N,N-dimethyltryptamine and N,N-diisopropyltryptamine in rats and mice. Front Neural Circuits 232 275 PMID: 24985890

Sher and DeVries (2012) A non-canonical pathway for mammalian blue-green color vision. Nat Neurosci 15 952 PMID: 22634728

Lee and Sherman (2012) Intrinsic modulators of auditory thalamocortical transmission. Hear Res 287 43 PMID: 22726616

Fuortes et al (2010) Distinctions between persistent and reversible group I mGluR-induced epileptiform burst prolongation. Epilepsia 51 1633 PMID: 20659148

Buchanan et al (2010) Facilitation of long-term potentiation by muscarinic M(1) receptors is mediated by inhibition of SK channels. Neuron 68 948 PMID: 21145007

Chen et al (2010) The glutamatergic compounds sarcosine and N-acetylcysteine ameliorate prepulse inhibition deficits in metabotropic glutamate 5 receptor knockout mice. Psychopharmacology (Berl) 209 343 PMID: 20217053

Bender et al (2006) Two coincidence detectors for spike timing-dependent plasticity in somatosensory cortex. J Neurosci 26 4166 PMID: 16624937

Proudfoot et al (2006) Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain. Curr Biol 16 1591 PMID: 16920620

Galici et al (2006) Biphenyl-indanone A, a positive allosteric modulator of the metabotropic glutamate receptor subtype 2, has antipsychotic- and anxiolytic-like effects in mice. J Pharmacol Exp Ther 318 173 PMID: 16608916

Choi et al (2005) Multiple receptors coupled to phospholipase C gate long-term depression in visual cortex. J Neurosci 25 11433 PMID: 16339037

Hulme et al (2012) Calcium-dependent but action potential-independent BCM-like metaplasticity in the hippocampus. J Neurosci 32 6785 PMID: 22593048

Citri et al (2010) Calcium binding to PICK1 is essential for the intracellular retention of AMPA receptors underlying long-term depression. J Neurosci 30 16437 PMID: 21147983

Adedoyin et al (2010) Endogenous N-acetylaspartylglutamate (NAAG) inhibits synaptic plasticity/transmission in the amygdala in a mouse inflammatory pain model. Mol Pain 6 60 PMID: 20860833

Wang et al (2004) Block of long-term potentiation by naturally secreted and synthetic amyloid beta-peptide in hippocampal slices is mediated via activation of the kinases c-Jun N-terminal kinase, cyclin-dependent kinase 5, and p38 mitogen-activated protein kinase as well a J Neurosci 24 3370 PMID: 15056716

Cao et al (2016) EXPRESS: Histone hyperacetylation modulates spinal type II metabotropic glutamate receptor alleviating stress-induced visceral hypersensitivity in female rats. Mol Pain 12 PMID: 27385724

Choi et al (2016) Multiple Drug Treatments That Increase cAMP Signaling Restore Long-Term Memory and Aberrant Signaling in Fragile X Syndrome Models. Front Behav Neurosci 10 136 PMID: 27445731

Johansson et al (2015) Activation of a temporal memory in purkinje cells by the mGluR7 receptor. Cell Rep. 13 1741 PMID: 26655894

Ren et al (2012) Intrathecal injection of metabotropic glutamate receptor subtype 3 and 5 agonist/antagonist attenuates bone cancer pain by inhibition of spinal astrocyte activation in a mouse model. Anesthesiology 116 122 PMID: 22123524

Sekizawa et al (2009) A novel postsynaptic group II metabotropic glutamate receptor role in modulating baroreceptor signal transmission. J Neurosci 29 11807 PMID: 19776267

Fujino and Oertel (2003) Bidirectional synaptic plasticity in the cerebellum-like mammalian dorsal cochlear nucleus. Proc Natl Acad Sci U S A 100 265 PMID: 12486245

Nishi et al (2003) Metabotropic mGlu5 receptors regulate adenosine A2A receptor signaling. Front Behav Neurosci 100 1322 PMID: 12538871

Moore et al (2003) Adenosine gates synaptic plasticity at hippocampal mossy fiber synapses. Proc Natl Acad Sci U S A 100 14397 PMID: 14608033

Dunn (2015) Photoreceptor ablation initiates the immediate loss of glutamate receptors in postsynaptic bipolar cells in retina. Elife 35 2423 PMID: 25673837

Mahler et al (2014) Modafinil attenuates reinstatement of cocaine seeking: role for cystine-glutamate exchange and metabotropic glutamate receptors. J Neurosci 19 49 PMID: 23017017

Case et al (2014) VGLUT3 does not synergize GABA/glycine release during functional refinement of an inhibitory auditory circuit. J Neurosci 8 140 PMID: 25505386

Chen et al (2014) Activation of mGluR2/3 underlies the effects of N-acetylcystein on amygdala-associated autism-like phenotypes in a valproate-induced rat model of autism. J Neurophysiol 8 219 PMID: 24987341

Hoshi et al (2013) Properties of the ON bistratified ganglion cell in the rabbit retina. J Comp Neurol 521 1497 PMID: 23047654

Trepanier et al (2013) Group II metabotropic glutamate receptors modify N-methyl-D-aspartate receptors via Src kinase. Sci Rep 3 926 PMID: 23378895

Jin et al (2011) Whereas short-term facilitation is presynaptic, intermediate-term facilitation involves both presynaptic and postsynaptic protein kinases and protein synthesis. Learn Mem 18 96 PMID: 21245210

Muto et al (2009) Site-specific unglycosylation to improve crystallization of the metabotropic glutamate receptor 3 extracellular domain. Proc Natl Acad Sci U S A 65 236 PMID: 19255473

Carlton et al (2009) Group II metabotropic glutamate receptor activation on peripheral nociceptors modulates TRPV1 function. Eur J Neurosci 1248 86 PMID: 19026992

Citri et al (2009) N-methyl-D-aspartate receptor- and metabotropic glutamate receptor-dependent long-term depression are differentially regulated by the ubiquitin-proteasome system. Neuropsychopharmacology 30 1443 PMID: 19821836

Lafourcade et al Molecular components and functions of the endocannabinoid system in mouse prefrontal cortex. PLoS One 2 e709 PMID: 17684555


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