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MTEP Hydrochloride 1186195-60-7

MTEP Hydrochloride 1186195-60-7

CAS No.: 1186195-60-7

MTEP HCl is a potent, noncompetitive and selective mGluR5 antagonist. MTEP HCl displays antidepressant and anxiolytic (a
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MTEP HCl is a potent, noncompetitive and selective mGluR5 antagonist. MTEP HCl displays antidepressant and anxiolytic (anti-anxiety) effects. MTEP HCl may be utilized in Parkinson's disease (PD) research.

Physicochemical Properties


Molecular Formula C11H9CLN2S
Molecular Weight 236.720559835434
Exact Mass 236.017
CAS # 1186195-60-7
Related CAS # MTEP;329205-68-7
PubChem CID 45073467
Appearance Light yellow to yellow solid powder
LogP 3.048
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 3
Rotatable Bond Count 2
Heavy Atom Count 15
Complexity 253
Defined Atom Stereocenter Count 0
InChi Key YCIOJDKGCWAHLR-UHFFFAOYSA-N
InChi Code

InChI=1S/C11H8N2S.ClH/c1-9-13-11(8-14-9)5-4-10-3-2-6-12-7-10;/h2-3,6-8H,1H3;1H
Chemical Name

2-methyl-4-(2-pyridin-3-ylethynyl)-1,3-thiazole;hydrochloride
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vitro Compared to MPEP, MTEP is less off-target and has a different selectivity for mGluR5 than mGluR1, while MPEP has no effect on other mGluR subtypes [1].
ln Vivo The catalepsy coefficient caused by haloperidol (0.5 mg/kg, i.p.) is inhibited by MTEP (0-5 mg/kg, i.p., once) [2]. MTEP (0.3-3 mg/kg, i.p., once) is in control.
Animal Protocol Animal/Disease Models: Male Wistar rats (215-315 g, 5-9/group) [2] Doses: 1, 3, and 5 mg/kg given Medication method: IP, inducing antidepressant-like effects in C57BL/6J mice [3]. One injection, 60 minutes after haloperidol (0.5 mg/kg/2 ml ip)
Experimental Results:Inhibition of haloperidol-induced rigor.

Animal/Disease Models: Male C57BL/6J mice (23-25 g) [3]
Doses: 0.3, 1 and 3 mg/kg
Route of Administration: intraperitoneal (ip) injection, 1 hour before test
Experimental Results: Dramatically diminished mice in the tail suspension test Immobility time (Tsim Sha Tsui) increased by 24%, 41% and 48% respectively. The efficacy of MTEP used at doses of 1 and 3 mg/kg was not Dramatically different from that of imipramine (20 mg/kg, i.p.) used as a positive standard.
References

[1]. Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP. CNS Drug Rev. 2006 Summer;12(2):149-66.

[2]. 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.

[3]. Potential antidepressant-like effect of MTEP, a potent and highly selective mGluR5 antagonist. Pharmacol Biochem Behav. 2005 Aug;81(4):901-6.

[4]. 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.


Solubility Data


Solubility (In Vitro) H2O : ~20 mg/mL (~84.49 mM)
Solubility (In Vivo) Solubility in Formulation 1: 100 mg/mL (422.44 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.2244 mL 21.1220 mL 42.2440 mL
5 mM 0.8449 mL 4.2244 mL 8.4488 mL
10 mM 0.4224 mL 2.1122 mL 4.2244 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.