LY 341495

Cat. No. 1209

LY 341495 C20H19NO5 [201943-63-7]

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Chemical Name: (2S)-2-Amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xanth-9-yl) propanoic acid

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
Solubility:
Soluble to 10 mM in DMSO with gentle warming and to 100 mM in 1.2eq. NaOH
Purity:
>98 %
Storage:
Store at RT
CAS No:
201943-63-7

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 / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
Select another batch:

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.

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.

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 bioavailability. J.Med.Chem. 41 358. PMID: 9464367.

If you know of a relevant reference for this product please let us know.

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

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.

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.

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

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

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

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

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.

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.

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

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.

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.

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.

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.

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

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.

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

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.

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.

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.

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

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.

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.

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.

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

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

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

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

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.

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

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

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.

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

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.

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

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

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

Do you know of a great paper that uses LY 341495 from Tocris? If so please let us know.show all ▼show less ▲

Keywords: 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, Tocris Bioscience, Glutamate (Metabotropic) Group II Receptor Antagonist products

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