MTEP Hydrochloride | CAS# 1186195-60-7 | mGlu antagonist

MTEP Hydrochloride
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 571355

CAS#: 1186195-60-7

Description: MTEP HCl is a potent and selective non-competitive mGlu5 antagonist/negative allosteric modulator. It displays anxiolytic and antidepressant activity and can cross the blood-brain barrier.

Chemical Structure

MTEP Hydrochloride

CAS# 1186195-60-7

Instruction

Theoretical Analysis

MedKoo Cat#: 571355
Name: MTEP Hydrochloride
CAS#: 1186195-60-7
Chemical Formula: C11H9ClN2S
Exact Mass: 236.02
Molecular Weight: 236.720
Elemental Analysis: C, 55.81; H, 3.83; Cl, 14.98; N, 11.83; S, 13.54

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 300
50mg	USD 900
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: MTEP

IUPAC/Chemical Name: 3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine hydrochloride

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

SMILES Code: CC1=NC(C#CC2=CC=CN=C2)=CS1.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 236.72 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Pałucha-Poniewiera A, Brański P, Wierońska JM, Stachowicz K, Sławińska A, Pilc A. The antidepressant-like action of mGlu5 receptor antagonist, MTEP, in the tail suspension test in mice is serotonin dependent. Psychopharmacology (Berl). 2014 Jan;231(1):97-107. PubMed PMID: 23958941.

2: Nagel J, Greco S, Parsons CG, Flik G, Tober C, Klein KU, Danysz W. Brain concentrations of mGluR5 negative allosteric modulator MTEP in relation to receptor occupancy--Comparison to MPEP. Pharmacol Rep. 2015 Jun;67(3):624-30. doi: 10.1016/j.pharep.2015.01.004. Epub 2015 Jan 22. PubMed PMID: 25933979.

3: Swedberg MD, Ellgren M, Raboisson P. mGluR5 antagonist-induced psychoactive properties: MTEP drug discrimination, a pharmacologically selective non-NMDA effect with apparent lack of reinforcing properties. J Pharmacol Exp Ther. 2014 Apr;349(1):155-64. doi: 10.1124/jpet.113.211185. Epub 2014 Jan 28. PubMed PMID: 24472725.

4: Domin H, Szewczyk B, Woźniak M, Wawrzak-Wleciał A, Śmiałowska M. Antidepressant-like effect of the mGluR5 antagonist MTEP in an astroglial degeneration model of depression. Behav Brain Res. 2014 Oct 15;273:23-33. doi: 10.1016/j.bbr.2014.07.019. Epub 2014 Jul 18. PubMed PMID: 25043733.

5: Handford CE, Tan S, Lawrence AJ, Kim JH. The effect of the mGlu5 negative allosteric modulator MTEP and NMDA receptor partial agonist D-cycloserine on Pavlovian conditioned fear. Int J Neuropsychopharmacol. 2014 Sep;17(9):1521-32. doi: 10.1017/S1461145714000303. Epub 2014 Mar 27. PubMed PMID: 24674862.

6: Pałucha-Poniewiera A, Szewczyk B, Pilc A. Activation of the mTOR signaling pathway in the antidepressant-like activity of the mGlu5 antagonist MTEP and the mGlu7 agonist AMN082 in the FST in rats. Neuropharmacology. 2014 Jul;82:59-68. doi: 10.1016/j.neuropharm.2014.03.001. Epub 2014 Mar 12. PubMed PMID: 24631968.

7: Zavala-Tecuapetla C, Kubová H, Otáhal J, Tsenov G, Mareš P. Age-dependent suppression of hippocampal epileptic afterdischarges by metabotropic glutamate receptor 5 antagonist MTEP. Pharmacol Rep. 2014 Oct;66(5):927-30. doi: 10.1016/j.pharep.2014.02.018. Epub 2014 Mar 13. PubMed PMID: 25150003.

8: Chapman AM, Taylor CA, Girling AJ. Are the UK systems of innovation and evaluation of medical devices compatible? The role of NICE's Medical Technologies Evaluation Programme (MTEP). Appl Health Econ Health Policy. 2014 Aug;12(4):347-57. doi: 10.1007/s40258-014-0104-y. PubMed PMID: 24934924.

9: Roohi N, Sarihi A, Shahidi S, Zarei M, Haghparast A. Microinjection of the mGluR5 antagonist MTEP into the nucleus accumbens attenuates the acquisition but not expression of morphine-induced conditioned place preference in rats. Pharmacol Biochem Behav. 2014 Nov;126:109-15. doi: 10.1016/j.pbb.2014.09.020. Epub 2014 Oct 2. PubMed PMID: 25284131.

10: Tichá K, Mikulecká A, Mareš P. Behavioral consequences of the mGlu5 receptor antagonist MTEP in immature rats. Pharmacol Biochem Behav. 2011 Oct;99(4):619-25. doi: 10.1016/j.pbb.2011.06.007. Epub 2011 Jun 15. PubMed PMID: 21703298.

11: Arndt DL, Johns KC, Dietz ZK, Cain ME. Environmental condition alters amphetamine self-administration: role of the MGluR₅ receptor and schedule of reinforcement. Psychopharmacology (Berl). 2015 Oct;232(20):3741-52. doi: 10.1007/s00213-015-4031-x. Epub 2015 Jul 28. PubMed PMID: 26211759; PubMed Central PMCID: PMC4667709.

12: McIldowie MJ, Gandy MN, Skelton BW, Brotchie JM, Koutsantonis GA, Spackman MA, Piggott MJ. Physical and crystallographic characterisation of the mGlu5 antagonist MTEP and its monohydrochloride. J Pharm Sci. 2010 Jan;99(1):234-45. doi: 10.1002/jps.21823. PubMed PMID: 19499574.

13: Brown RM, Stagnitti MR, Duncan JR, Lawrence AJ. The mGlu5 receptor antagonist MTEP attenuates opiate self-administration and cue-induced opiate-seeking behaviour in mice. Drug Alcohol Depend. 2012 Jun 1;123(1-3):264-8. doi: 10.1016/j.drugalcdep.2011.11.002. Epub 2011 Nov 29. PubMed PMID: 22129842.

14: Domin H, Zięba B, Gołembiowska K, Kowalska M, Dziubina A, Śmiałowska M. Neuroprotective potential of mGluR5 antagonist MTEP: effects on kainate-induced excitotoxicity in the rat hippocampus. Pharmacol Rep. 2010 Nov-Dec;62(6):1051-61. PubMed PMID: 21273662.

15: Keck TM, Zou MF, Bi GH, Zhang HY, Wang XF, Yang HJ, Srivastava R, Gardner EL, Xi ZX, Newman AH. A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats. Addict Biol. 2014 Mar;19(2):195-209. doi: 10.1111/adb.12086. Epub 2013 Sep 4. PubMed PMID: 24001208; PubMed Central PMCID: PMC3942387.

16: Pomierny-Chamioło L, Poleszak E, Pilc A, Nowak G. NMDA but not AMPA glutamatergic receptors are involved in the antidepressant-like activity of MTEP during the forced swim test in mice. Pharmacol Rep. 2010 Nov-Dec;62(6):1186-90. PubMed PMID: 21273676.

17: Martin-Fardon R, Baptista MA, Dayas CV, Weiss F. Dissociation of the effects of MTEP [3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]piperidine] on conditioned reinstatement and reinforcement: comparison between cocaine and a conventional reinforcer. J Pharmacol Exp Ther. 2009 Jun;329(3):1084-90. doi: 10.1124/jpet.109.151357. Epub 2009 Mar 3. PubMed PMID: 19258516; PubMed Central PMCID: PMC2683783.

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