MTEP

MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research[1][2][3][4].

Signaling Pathways >> GPCR/G Protein >> mGluR

Research Areas >> Neurological Disease

mGluR5:5 nM (IC50)

mGluR5:16 nM (Ki)

MTEP 对 mGluR5 的选择性高于 mGluR1，对其他 mGluR 亚型没有影响，并且比 MPEP (HY-14609A) 有更少的脱靶效应[1]。

MTEP (0-5 mg/kg, 腹腔注射, 一次) 抑制由 Haloperidol (HY-14538) (0.5 mg/kg, 腹腔注射)诱导的僵直症[2]。 MTEP (0.3-3 mg/kg, 腹腔注射, 一次) 在雄性 C57BL/6J 小鼠中诱导抗抑郁样作用[3]。 Animal Model: Male Wistar rats (215-315 g, 5-9/group)[2] Dosage: 1, 3 and 5 mg/kg Administration: IP, once, injected 60 min after Haloperidol (HY-14538) (0.5 mg/kg/2 ml i.p.) Result: Inhibited the catalepsy induced by Haloperidol (HY-14538). Animal Model: Male C57BL/6J mice (23-25 g)[3] Dosage: 0.3, 1 and 3 mg/kg Administration: IP, 1 h before the test Result: Significantly decreased the immobility time of mice in the tail suspension test (TST) by 24%, 41% and 48%, respectively. The efficacy of MTEP used at doses of 1 and 3 mg/kg was not significantly different from that of Imipramine (HY-B1490A) (20 mg/kg, ip), used as a positive standard.

[1]. Lea PM 4th, et al. Metabotropic glutamate receptor subtype 5 antagonists MPEP and MTEP. CNS Drug Rev. 2006 Summer;12(2):149-66.  

[2]. Ossowska K, et al. 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]. Pałucha A, et al. Potential antidepressant-like effect of MTEP, a potent and highly selective mGluR5 antagonist. Pharmacol Biochem Behav. 2005 Aug;81(4):901-6.  

[4]. Klodzinska A, 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.