1186195-60-7

1186195-60-7 structure

Name: MTEP (hydrochloride)
Chemical Name: 2-methyl-4-(2-pyridin-3-ylethynyl)-1,3-thiazole,hydrochloride
CAS Number: 1186195-60-7
Molecular Formula: C₁₁H₉ClN₂S
Molecular Weight: 236.721
Catalog: Research Areas Neurological Disease
Create Date: 2016-02-07 09:45:53
Modify Date: 2024-01-05 17:59:52
MTEP Hcl is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively. IC50 Value: 5 nM [1]Target: mGluR5MTEP occupied mGlu5 receptors in a dose-dependent manner with essentially full receptor occupancy at the highest dose tested (10 mg/kg, i.p.). At doses appropriate for mGlu5 receptor-mediated effects, MTEP significantly reduced fear-potentiated startle and increased punished responding in a modified Geller-Seifter conflict model consistent with an anxiolytic-like profile. MTEP decreased unpunished responding to a lesser extent than diazepam and had no effect on rotarod performance when administered either alone or in combination with ethanol. Repeated dosing with MTEP in this model eliminated the increase in punished responding observed with acute dosing.

Name	2-methyl-4-(2-pyridin-3-ylethynyl)-1,3-thiazole,hydrochloride
Synonyms	3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]pyridine hydrochloride (1:1) CS-1249 MTEP hydrochloride Pyridine, 3-[2-(2-methyl-4-thiazolyl)ethynyl]-, hydrochloride (1:1) 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pyridine hydrochloride MTEP hydrochloride\|\|MTEP MTEP (hydrochloride)

Description	MTEP Hcl is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively. IC50 Value: 5 nM [1]Target: mGluR5MTEP occupied mGlu5 receptors in a dose-dependent manner with essentially full receptor occupancy at the highest dose tested (10 mg/kg, i.p.). At doses appropriate for mGlu5 receptor-mediated effects, MTEP significantly reduced fear-potentiated startle and increased punished responding in a modified Geller-Seifter conflict model consistent with an anxiolytic-like profile. MTEP decreased unpunished responding to a lesser extent than diazepam and had no effect on rotarod performance when administered either alone or in combination with ethanol. Repeated dosing with MTEP in this model eliminated the increase in punished responding observed with acute dosing.
Related Catalog	Research Areas >> Neurological Disease
References	[1]. Nicolas Morin, Laurent Grégoire, Baltazar Gomez-Mancilla, et al. Effect of the metabotropic glutamate receptor type 5 antagonists MPEP and MTEP in parkinsonian monkeys. Neuropharmacology. 2010, 58 (7): 981-986 [2]. Tom H. Johnston, Susan H. Fox, Matthew J. McIldowie, et al. Reduction of l-DOPA-Induced Dyskinesia by the Selective Metabotropic Glutamate Receptor 5 Antagonist 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]pyridine in the 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyri [3]. Bradbury MJ, Campbell U, Giracello D, et al. Metabotropic glutamate receptor mGlu5 is a mediator of appetite and energy balance in rats and mice. J Pharmacol Exp Ther. 2005 Apr;313(1):395-402. [4]. Klodzinska A, Tatarczyńska E, Chojnacka-Wójcik E 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. [5]. Brodkin J, Bradbury M, Busse C, et al. Reduced stress-induced hyperthermia in mGluR5 knockout mice. Eur J Neurosci. 2002 Dec;16(11):2241-4.

Molecular Formula	C₁₁H₉ClN₂S
Molecular Weight	236.721
Exact Mass	236.017502
PSA	54.02000
LogP	3.04830
Storage condition	2-8℃

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