MTEP 是一种有效的、非竞争性和高选择性的mGluR5拮抗剂。MTEP 表现出抗抑郁和抗焦虑的作用。MTEP 可以用于帕金森疾病的研究。
生物活性 | MTEP is a potent, non-competitive and highly selectivemGluR5antagonist, with anIC50of 5 nM and aKiof 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research[1][2][3][4]. |
IC50& Target | mGluR5 5 nM (IC50) | mGluR5 16 nM (Ki) |
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体外研究 (In Vitro) | 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]。
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体内研究 (In Vivo) | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |