LY341495 |
| Katalog-Nr.GC14555 |
Selective antagonist of mGluR2 and mGluR3
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 201943-63-7
Sample solution is provided at 25 µL, 10mM.
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LY341495 is a highly potent and selective antagonist of group II metabotropic glutamate receptors with IC50 values of 21 nM and 14 nM for mGlu2 and mGlu3 receptors, respectively [1].
Glutamate is the major excitatory neurotransmitter that regulates neuronal plasticity and maintains fast synaptic transmission. The aberrant glutamate pathway has been found in a serious of neurological?problems, such as cognitive disorders, epilepsy and AD. As a selective inhibitor of group II metabotropic glutamate receptors (including mGlu2 and mGlu3), LY341495 acts as a competitive antagonist to regulate the transmission of glutamate [1 and 2].
In the functional assays, LY341495 at concentrations of 0.1 μM and 30 nM completely reversed the ACPD-induced inhibition of cAMP formation which was stimulated by forskolin in mGlu2 expressing cells and mGlu3 expressing cells, respectively. In RGT cells expressing group III mGlu receptors (mGlu4, 6, 7 and 8), LY341495 showed significant reversion of L-AP4-inhibited cAMP formation stimulated by forskolin. For mGlu4a, 7a and 8, the IC50 value of LY341495 were 22, 0.99 and 0.173 μM, respectively, which were 5 to 1000-fold higher than that for mGlu2 and mGlu3. For the group I mGlu receptors (mGlu1a and 5a), the IC50 values were 6.8 and 8.2 μM, respectively. Besides that, LY341495 was found to reversibly eliminate the long-term synaptic depression induced by DHPG in rats’ hippocampal slices [1 and 2].
In animal experiments, LY341495 was found to have effects on the post-training recognition memory. It was reported that the administration of LY341495 at different doses showed different efficacies on rats’ recognition memory. Rats treated with LY341495 at doses of 0.3, 1 and 3 mg/kg displayed a significant lower level of discrimination while LY341495 at doses of 0.05 and 0.1 mg/kg exerted a reversion of the recognition memory extinction and showed no impairment of the recognition memory [3].
References:
[1] Kingston A E, Ornstein P L, Wright R A, et al. LY341495 is a nanomolar potent and selective antagonist of group II metabotropic glutamate receptors. Neuropharmacology, 1998, 37(1): 1-12.
[2] Fitzjohn S M, Bortolotto Z A, Palmer M J, et al. The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology, 1998, 37(12): 1445-1458.
[3] Pitsikas N, Kaffe E, Markou A. The metabotropic glutamate 2/3 receptor antagonist LY341495 differentially affects recognition memory in rats. Behavioural brain research, 2012, 230(2): 374-379.
| Cell experiment [1]: | |
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Cell lines |
U87 cell lines |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
72h; 1 μM |
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Applications |
It is well established that U87 cells proliferate in a glutamate-dependent manner and drugs LY341495, an inhibitor of metabotropic glutamate receptor have been shown to inhibit proliferation of glioma cells. The result shown that Iressa in combination with LY341495 is effective in inhibiting proliferation. |
| Animal experiment [2]: | |
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Animal models |
Male 6-week-old Sprague-Dawley rats |
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Dosage form |
3 mg/kg; intraperitoneal injection |
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Applications |
We tested the anti-immobility effect of LY341495 in the forced swim test (FST). LY341495 significantly decreased the immobility behavior (F(3,36)=3.05; P |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Yelskaya Z, Carrillo V, Dubisz E, et al. Synergistic Inhibition of Survival, Proliferation, and Migration of U87 Cells with a Combination of LY341495 and Iressa[J]. PloS one, 2013, 8(5): e64588. [2] Koike H1, Chaki S2. Requirement of AMPA receptor stimulation for the sustained antidepressant activity of ketamine and LY341495 during the forced swim test in rats. Behav Brain Res. 2014 Sep 1;271:111-5. doi: 10.1016/j.bbr.2014.05.065. Epub 2014 Jun 5. |
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| Cas No. | 201943-63-7 | SDF | |
| Chemical Name | (1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]cyclopropane-1-carboxylic acid | ||
| Canonical SMILES | C1C(C1C(CC2C3=CC=CC=C3OC4=CC=CC=C24)(C(=O)O)N)C(=O)O | ||
| Formula | C20H19NO5 | M.Wt | 353.38 |
| Löslichkeit | 0.5 mg/ml in DMSO, 0.1 mg/ml in methanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8298 mL | 14.1491 mL | 28.2981 mL |
| 5 mM | 0.566 mL | 2.8298 mL | 5.6596 mL |
| 10 mM | 0.283 mL | 1.4149 mL | 2.8298 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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