MTEP hydrochloride - CAS 1186195-60-7
Catalog number: 1186195-60-7
Category: Inhibitor
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Glutamate, the major excitatory neurotransmitter in the brain, acts on both ionotropic and metabotropic glutamate receptors. Excessive metabotropic glutamate receptor (mGluR) transmission has been linked to epilepsy, ischemia, pain, anxiety, and depression. Eight subtypes (1-8) and multiple splice variants of the mGluR have been identified and grouped based on their pharmacological properties. Group I mGluRs (subtypes 1 and 5) activate the phosphatidyl inositol pathway, while Group II (2 and 3) and Group III (4, 6, 7, and 8) inhibit adenylyl cyclase. MTEP is a negative allosteric modulator of the mGlu5a receptor subtype (Ki = 42 nM; IC50 = 110 nM). MTEP at 0.3 mg/kg produces antidepressant effects in several rodent models of depression. It also demonstrates neuroprotective potential by preventing excitotoxic neuronal damage when administered through either intrahippocampal or intraperitoneal injection. Additionally, MTEP demonstrates an anxiolytic-like phenotype in rodent models similar to that of benzodiazepines while lacking undesirable sedative and addictive effects.
3-((2-Methyl-1,3-thiazol-4-yl)ethyn-yl)pyridine hydrochloride; MTEP
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1.Interactions of CB1 and mGlu5 receptor antagonists in food intake, anxiety and memory models in rats.
Varga B1, Kassai F, Gyertyán I. Pharmacol Biochem Behav. 2012 Dec;103(2):425-30. doi: 10.1016/j.pbb.2012.09.016. Epub 2012 Sep 28.
CB(1) receptor antagonists proved to be effective anti-obesity drugs, however, their depressive and anxiogenic effects became also evident. Finding solution to overcome these psychiatric side effects is still in focus of research. Based on the available clinical and preclinical results we hypothesized that the combination of CB(1) and mGlu(5) receptor antagonisms may result in a pharmacological intervention, where the anxiolytic mGlu(5) receptor inhibition may counteract the anxiogenic psychiatric side effects of CB(1) antagonism, while CB(1) antagonism may ameliorate the memory impairing effect of mGlu(5) receptor antagonism. Further, the two components will synergistically interact in blocking food-intake and reducing obesity. For testing the interaction of mGlu(5) and CB(1) receptor antagonism MTEP [3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]pridine; SIB-1757, 6-methyl-2-(phenylazo)-3-pyridinol)] (mGlu(5) antagonist) and rimonabant [(5-(4-Chlorophenyl)-1-(2,4-dichloro-phenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide)hydrochloride] (CB(1) antagonist) were used.
2.Activation of lateral hypothalamic mGlu1 and mGlu5 receptors elicits feeding in rats.
Charles JR1, Duva MA2, Ramirez GJ3, Lara RL3, Yang CR4, Stanley BG5. Neuropharmacology. 2014 Apr;79:59-65. doi: 10.1016/j.neuropharm.2013.10.033. Epub 2013 Nov 9.
Metabotropic glutamate receptors (mGluRs) have been popular drug targets for a variety of central nervous system (CNS) disease models, ranging from seizures to schizophrenia. The current study aimed to determine whether mGluRs participate in lateral hypothalamic (LH) stimulation of feeding. To this end, we used satiated adult male Sprague-Dawley rats stereotaxically implanted with indwelling bilateral LH guide cannulas to determine if injection of (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid (ACPD), a broad mGluR group I and II agonist, would elicit feeding. Administration of 100 nmol ACPD induced feeding with a short latency. Similarly, unilateral LH injection of the selective mGluR group I agonist (S)-3,5-dihydroxyphenylglycine (DHPG) elicited significant feeding beginning 60 min postinjection and continuing until 4 h postinjection. Administration of the mGluR5 agonist, (RS)-2-chloro-5-hydroxyphenylglycine (CHPG) produced a smaller delayed feeding response.
3.Environmental condition alters amphetamine self-administration: role of the MGluR₅ receptor and schedule of reinforcement.
Arndt DL1, Johns KC, Dietz ZK, Cain ME. Psychopharmacology (Berl). 2015 Oct;232(20):3741-52. doi: 10.1007/s00213-015-4031-x. Epub 2015 Jul 28.
RATIONALE: Evidence suggests that differential rearing influences the function of a receptor subtype critical for maintaining glutamate homeostasis. Maintaining homeostatic glutamatergic function may be an important protector against drug abuse.
4.Non-competitive metabotropic glutamate 1 receptor antagonists block activity of slowly adapting type I mechanoreceptor units in the rat sinus hair follicle.
Cahusac PM1, Mavulati SC. Neuroscience. 2009 Oct 20;163(3):933-41. doi: 10.1016/j.neuroscience.2009.07.015. Epub 2009 Jul 28.
Previous studies suggested that Group I metabotropic glutamate (mGlu) receptors play a role in mechanotransduction processes of slowly adapting type I mechanoreceptors. Using an isolated rat sinus hair follicle preparation we tested a range of compounds. Surprisingly, only non-competitive mGlu1 receptor antagonists produced profound and long-lasting depression of mechanically evoked firing. 6-Amino-N-cyclohexyl-N,3-dimethylthiazolo[3,2-alpha]benzimidazole-2-carboxamide hydrochloride (YM-298198) had an IC(50) of 8.7 muM (95% CI 5.7 to 13.2 microM), representing the most potent known blocker of type I mechanoreceptors. The derivative 6-amino-N-cyclohexyl-3-methylthiazolo[3,2-alpha]benzimidazole-2-carboxamide hydrochloride (desmethyl YM-298198) had a comparable potency. Another compound 7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylate ethyl ester (CPCCOEt) had a similar depressant effect, although it was less potent with an approximate IC(50) of 100 microM.
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CAS 1186195-60-7 MTEP hydrochloride

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