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编 号:F321568
分子式:C11H8N2S
分子量:200.26
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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. MTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

体内研究:
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。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。Animal Model:Male Wistar rats (215-315 g, 5-9/group)
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)
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.

体外研究:
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。
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