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LY 341495 is a novel, potent and selective orthosteric antagonist of the metabotropic glutamate receptors (mGluR) with IC50s of 2.9 nM, 10 nM, 170 nM for mGluR-2, mGluR-3, mGluR-8, respectively. It has shown antidepressant effects in animal models, increased the behavioral effects of hallucinogenic drugs in animal tests, increased the analgesic effects of μ-opioid agonists, and modulated dopamine receptor function. It has been used in scientific research in a variety of areas.
| Targets |
mGluR1a ( IC50 = 7.8 μM ); mGluR2 ( IC50 = 21 nM ); mGluR3 ( IC50 = 14 nM ); mGluR4 ( IC50 = 22 μM ); mGluR5a ( IC50 = 8.2 μM ); mGluR7 ( IC50 = 990 nM ); mGluR8 ( IC50 = 170 nM )
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| ln Vivo |
LY341495 (0.3, 1 and 3 mg/kg, ip) exhibits lower levels of insight into the state [1]. LY341495 (3.0 mg/kg) reduced Dvl-2, pGSK-3α/β and β-catenin protein levels, but Dvl-1, Dvl-3 and GSK-3α/β were not activated in PFC and STR. Compared with the mGlu2/3 stimulant LY379268, LY341495 generally produces just the right effect after fast and fast[2]. c-Fos expression induced by LY341495 (3 mg/kg, i.p., 2.5 hours) was not altered in either KO brain. In mGluR3-KO, LY341495 has little activity in the central extended amygdala [central amygdala] nucleus, nucleus of cancellation (CeL) and bed nucleus of stria terminalis, dorsal nucleus (BSTLD) [3].
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| Animal Protocol |
Six experimental groups (each with ten rats) are created by randomly assigning the rats: vehicle and 0.05, 0.1, 0.3, 1, and 3 mg/kg LY341475. The LY341495 doses are selected on the basis of results from previous Published studies that evaluated the effects of this compound on cognition. Training: Two 2-minute trials were given to the rats during the training session. Right after T1, the animals are given either LY341495 or the vehicle. Given that untreated control rats in these experiments still have intact recognition memory, an ITI of one hour is employed with a 2-min trial duration.
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| References |
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| Molecular Formula |
C20H19NO5
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| Molecular Weight |
353.36856
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| Exact Mass |
353.13
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| Elemental Analysis |
C, 67.98; H, 5.42; N, 3.96; O, 22.64
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| CAS # |
201943-63-7
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| Related CAS # |
(Rac)-LY341495
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| Appearance |
Solid powder
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| SMILES |
C1[C@@H]([C@H]1[C@@](CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O
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| InChi Key |
VLZBRVJVCCNPRJ-KPHUOKFYSA-N
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| InChi Code |
InChI=1S/C20H19NO5/c21-20(19(24)25,15-9-13(15)18(22)23)10-14-11-5-1-3-7-16(11)26-17-8-4-2-6-12(14)17/h1-8,13-15H,9-10,21H2,(H,22,23)(H,24,25)/t13-,15-,20-/m0/s1
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| Chemical Name |
(1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropane-1-carboxylic acid
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| Synonyms |
LY 341495; LY-341495; LY341495
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~6 mg/mL (~17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.6 mg/mL (1.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8299 mL | 14.1495 mL | 28.2990 mL | |
| 5 mM | 0.5660 mL | 2.8299 mL | 5.6598 mL | |
| 10 mM | 0.2830 mL | 1.4149 mL | 2.8299 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Results from the novel object recognition test that involved a session that consisted of two 2-min trials and an 1 h ITI (see text for details).Behav Brain Res.2012 May 1;230(2):374-9. |
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 Results from the novel object recognition test that involved a session that consisted of two 2-min trials and a 24 h ITI (see text for details).Behav Brain Res.2012 May 1;230(2):374-9. |
 Results from the novel object recognition test that consisted of one 5-min trial, one 2-min trial, and a 24 h ITI (see text for details).Behav Brain Res.2012 May 1;230(2):374-9. |
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