329205-68-7
329205-68-7 structure
- Name: MTEP
- Chemical Name: 2-methyl-4-(2-pyridin-3-ylethynyl)-1,3-thiazole
- CAS Number: 329205-68-7
- Molecular Formula: C11H8N2S
- Molecular Weight: 200.26000
- Catalog: Signaling Pathways GPCR/G Protein mGluR
- Create Date: 2017-06-21 00:13:11
- Modify Date: 2024-02-04 16:01:09
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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[1][2][3][4].
| Name | 2-methyl-4-(2-pyridin-3-ylethynyl)-1,3-thiazole |
|---|---|
| Synonyms |
IN1238
3-((2-Methyl-1,3-thiazol-4-yl)ethynyl)pyridine MTEP mGluR5 Antagonist,MTEP |
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
mGluR5:5 nM (IC50) mGluR5:16 nM (Ki) |
| 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]。 |
| 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. |
| References |
| Molecular Formula | C11H8N2S |
|---|---|
| Molecular Weight | 200.26000 |
| Exact Mass | 200.04100 |
| PSA | 54.02000 |
| LogP | 2.24630 |
| Storage condition | 2-8°C |