MTEP
Based on 3 publication(s) in Google Scholar
MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research. MTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Pureté: 99.91%
- CAS No.: 329205-68-7
- Formule: C11H8N2S
- Masse moléculaire:200.26
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MTEP
More
Activité biologique
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mGluR5 5 nM (IC50) |
mGluR5 16 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
0.462 μM
Compound: 4
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Antagonist activity against mGluR5 expressed in CHO cells assessed as inhibition of agonist-induced phosphoinositide hydrolysis
Antagonist activity against mGluR5 expressed in CHO cells assessed as inhibition of agonist-induced phosphoinositide hydrolysis
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[PMID: 16678408] |
| CHO | IC50 |
462 nM
Compound: 22
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Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5a
Activity in agonist-induced phosphoinositide hydrolysis in CHO cells expressing mGluR5a
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[PMID: 16451073] |
| HEK293 | IC50 |
12 nM
Compound: MTEP
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Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
Negative allosteric modulation of human mGluR5 expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
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[PMID: 23434029] |
| HEK293 | IC50 |
5 nM
Compound: MTEP
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Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization
Antagonist activity at rat mGluR5 expressed in human HEK-293 cells assessed as inhibition of glutamate-induced intracellular calcium mobilization
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[PMID: 21546249] |
| HEK293-A | IC50 |
110 nM
Compound: 2, MTEP
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Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 production by ELISA
Inverse agonist activity at rat mGluR5 expressed in HEK293A cells coexpressing Gqalpha assessed as inhibition of quisqualic-induced D-myo-inositol 1 production by ELISA
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[PMID: 22924094] |
| HEK293-A | IC50 |
13.6 nM
Compound: 2
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Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay
Antagonist activity at rat mGluR5 expressed in HEK293A cells assessed as glutamate-induced calcium flux preincubated for 140 sec before glutamate challenge by calcium fluorescence assay
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[PMID: 19445453] |
MTEP (0.3-3 mg/kg, intraperitoneal injection, once) induces antidepressant-like effects in male C57BL/6J mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (215-315 g, 5-9/group)[2]
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Dosage:1, 3 and 5 mg/kg
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Administration:IP, once, injected 60 min after Haloperidol (HY-14538) (0.5 mg/kg/2 ml i.p.)
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Result:Inhibited the catalepsy induced by Haloperidol (HY-14538).
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Animal Model:Male C57BL/6J mice (23-25 g)[3]
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Dosage:0.3, 1 and 3 mg/kg
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Administration:IP, 1 h before the test
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Result:Significantly decreased the immobility time of mice in the tail suspension test (TST) by 24%, 41% and 48%, respectively. The efficacy of MTEP used at doses of 1 and 3 mg/kg was not significantly different from that of Imipramine (HY-B1490A) (20 mg/kg, ip), used as a positive standard.
Chemical Information
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CAS No. 329205-68-7
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Appearance Solid
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Masse moléculaire 200.26
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Formule C11H8N2S
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Color White to off-white
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SMILES
CC1=NC(C#CC2=CC=CN=C2)=CS1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Sci Adv
Loss of schizophrenia-related miR-501-3p in mice impairs sociability and memory by enhancing mGluR5-mediated glutamatergic transmission. [Abstract]2022 Aug 19;8(33):eabn7357. PMID: 35984881 -
Neurochem Int
Red nucleus mGluR1 and mGluR5 facilitate the development of neuropathic pain through stimulating the expressions of TNF-α and IL-1β. [Abstract]2024 Sep:178:105786. PMID: 38843952 -
Psychopharmacology (Berl)
2024 Jul;241(7):1399-1415. PMID: 38459971
Solvant et solubilité
DMSO : 100 mg/mL (499.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Lea PM 4th, et al. Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP. CNS Drug Rev. 2006 Summer;12(2):149-66. [Content Brief]
[2]. Ossowska K, et al. MTEP, a new selective antagonist of the metabotropic glutamate receptor subtype 5 (mGluR5), produces antiparkinsonian-like effects in rats. Neuropharmacology. 2005 Sep;49(4):447-55. [Content Brief]
[3]. Pałucha A, et al. Potential antidepressant-like effect of MTEP, a potent and highly selective mGluR5 antagonist. Pharmacol Biochem Behav. 2005 Aug;81(4):901-6. [Content Brief]
[4]. Klodzinska A, et al. Anxiolytic-like effects of MTEP, a potent and selective mGlu5 receptor agonist does not involve GABA(A) signaling. Neuropharmacology. 2004 Sep;47(3):342-50. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.9935 mL | 24.9675 mL | 49.9351 mL | 124.8377 mL |
| 5 mM | 0.9987 mL | 4.9935 mL | 9.9870 mL | 24.9675 mL | |
| 10 mM | 0.4994 mL | 2.4968 mL | 4.9935 mL | 12.4838 mL | |
| 15 mM | 0.3329 mL | 1.6645 mL | 3.3290 mL | 8.3225 mL | |
| 20 mM | 0.2497 mL | 1.2484 mL | 2.4968 mL | 6.2419 mL | |
| 25 mM | 0.1997 mL | 0.9987 mL | 1.9974 mL | 4.9935 mL | |
| 30 mM | 0.1665 mL | 0.8323 mL | 1.6645 mL | 4.1613 mL | |
| 40 mM | 0.1248 mL | 0.6242 mL | 1.2484 mL | 3.1209 mL | |
| 50 mM | 0.0999 mL | 0.4994 mL | 0.9987 mL | 2.4968 mL | |
| 60 mM | 0.0832 mL | 0.4161 mL | 0.8323 mL | 2.0806 mL | |
| 80 mM | 0.0624 mL | 0.3121 mL | 0.6242 mL | 1.5605 mL | |
| 100 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2484 mL |
MTEP Related Classifications
HY-13206A Related Classifications
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