MTEP (hydrochloride)

Names

[ Name ]:
MTEP (hydrochloride)

[Synonym ]:
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)

Biological Activity

[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.

[Related Small Molecules]