MTEP

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MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC₅₀ of 5 nM and a K_i 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.

For research use only. We do not sell to patients.

MTEP Chemical Structure

CAS No. : 329205-68-7

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Other In-stock Forms of MTEP:

MTEP hydrochloride

Other Forms of MTEP:

MTEP hydrochloride In-stock

3 Publications Citing Use of MCE MTEP

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

Biological Activity
Purity & Documentation
References
Customer Review

Description

MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC₅₀ of 5 nM and a K_i of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research^[1]^[2]^[3]^[4]. 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.

IC₅₀ & Target

mGluR5

5 nM (IC₅₀)

mGluR5

16 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	12 nM Compound: MTEP	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	[PMID: 23434029]
HEK293-A	IC₅₀	110 nM Compound: 2, MTEP	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	[PMID: 22924094]
HEK293-A	IC₅₀	13.6 nM Compound: 2	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	[PMID: 19445453]

In Vitro

MTEP shows highly selective for mGluR5 over mGluR1, has no effect on other mGluR subtypes, and has fewer off-target effects than MPEP (HY-14609A)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MTEP (0-5 mg/kg, i.p., once) inhibits the catalepsy induced by Haloperidol (HY-14538) (0.5 mg/kg/2 ml i.p.)^[2].
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.

Animal Model:	Male Wistar rats (215-315 g, 5-9/group)^[2]
Dosage:	1, 3 and 5 mg/kg
Administration:	IP, once, injected 60 min after Haloperidol (HY-14538) (0.5 mg/kg/2 ml i.p.)
Result:	Inhibited the catalepsy induced by Haloperidol (HY-14538).

Animal Model:	Male C57BL/6J mice (23-25 g)^[3]
Dosage:	0.3, 1 and 3 mg/kg
Administration:	IP, 1 h before the test
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.

Molecular Weight

200.26

Formula

C₁₁H₈N₂S

CAS No.

329205-68-7

SMILES

CC1=NC(C#CC2=CC=CN=C2)=CS1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

MTEP Related Classifications

Neurological Disease

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
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C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MTEP329205-68-7mGluRMetabotropic glutamate receptorsAntidepressantanxiolytic-likeParkinson's diseaseInhibitorinhibitorinhibit

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