2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. YM-202074

YM-202074 是一种具有高亲和力的选择性的变构代谢型谷氨酸受体1型 (mGluR1) 拮抗剂。YM-202074结合大鼠 mGluR1 的变构位点，Ki 值为 4.8 nM。YM-202074 也能抑制 mGluR1 介导的大鼠小脑颗粒细胞肌醇磷酸的产生，IC50 值为 8.6 nM。YM-202074 在短暂性大脑中动脉 (tMCA) 闭塞大鼠模型中具有强效的神经保护作用。

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YM-202074

YM-202074 Chemical Structure

CAS No. : 299900-83-7

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YM-202074 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models[1].

IC50 & Target

rat mGluR1

4.8 nM (Ki)

体外研究
(In Vitro)

YM-202074 显著抑制大鼠小脑颗粒细胞中 mGluR1 介导的肌醇磷酸生成，IC50 为 8.6 nM[1]。
YM-202074 显示出对其他 mGluR 的特异性选择性，例如在 HEK 细胞和 CHO 细胞中，对 mGluR2、mGluR3、mGluR4a、mGluR6 或 mGluR7b (≤ 10 μM) 既无激动剂也无拮抗剂活性，但对 mGluR5 (10 μM) 具有反向激动剂活性[1]。
YM-202074 对离子型谷氨酸受体 (≤ 10 μM) 没有亲和力，对少数受体有中等程度的脱靶活性，例如对肾上腺素 α2C 受体、多巴胺转运体、乙酰胆碱 M2/M4 受体、sigma2 受体、钠通道位点 2 的抑制率 均 >60%，对其他 74 个位点的抑制率 ≤ 50%[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

YM-202074 相关抗体:
体内研究
(In Vivo)

YM-202074 (静脉输注，5 mg/kg/h 输注 8 小时，或 20 mg/kg/h 输注 0.5 小时，随后 5 mg/kg/h 输注 7.5 小时) 可迅速到达脑部，在 12 分钟内达到约 0.3 μM 的游离浓度，并以 20 mg/kg/h 输注 0.5 小时的负荷剂量输注，在 1.5 小时内达到稳态[1]。
YM-202074 (静脉输注，10-20 mg/kg/h 输注 0.5 小时，随后 2.5-5 mg/kg/h 输注 0.5-6 小时) 在 tMCA 闭塞大鼠模型中可提供不受低温等非特异性因素影响的神经保护作用，且未观察到显著的生理变化[1]。
YM-202074 (静脉输注，10-20 mg/kg/h，持续 0.5 小时，随后 2.5-5 mg/kg/h，持续 23.5 小时) 剂量依赖性地改善 tMCA 闭塞大鼠模型中的神经功能缺损，并减少半球和皮质的梗死体积，高剂量时疗效更佳[1]。
YM-202074 (静脉输注，20 mg/kg/h，持续 0.5 小时，随后在 tMCA 闭塞后 2 或 3 小时至 24 小时以 5 mg/kg/h 输注) 在 tMCA 闭塞大鼠模型中缺血发生 2 小时后给药，能显著维持神经保护作用[1]。
YM-202074 (静脉输注，20 mg/kg/h，持续 0.5 小时，随后在 tMCA 闭塞后 2 小时至 24 小时以 5 mg/kg/h 输注) 在 tMCA 闭塞大鼠模型中在缺血发生后 1 周给药，显著维持神经功能缺损的改善和梗死体积的减少以及大鼠体重的增加[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SD rats firstly given a left jugular vein cannulation at the dorsal neck with chloral hydrate anesthesia (i.p., 350 mg/kg,), and 24 h later, a 3-0 poly-L-lysine-coated suture was advanced about 17 mm intracranially from the common carotid artery bifurcation via the right and internal external carotid artery with halothane (0.5-1.5%) for 3 h[1].
Dosage: 10 or 20 mg/kg/h (loading infusion), 2.5 or 5 mg/kg/h (maintenance infusion)
Administration: i.v. infusion, loading infusion for 0.5 h followed by maintenance infusion for 23.5 h
Result: Dose-dependently improved neurological deficit and reduces the infarct volume in both the hemisphere and cortex in tMCA occlusion rat models.
Significantly reduced infarct volume in the hemisphere and the cortex by 55% and 70%, and improved neurological scores in tMCA occlusion rat models with 20 mg/kg/h for 0.5 h followed by 5 mg/kg/h for 23.5 h.
Animal Model: Male SD rats firstly given a left jugular vein cannulation at the dorsal neck with chloral hydrate Anesthesia (i.p., 350 mg/kg,), and24 h later, a 3-0 poly-L-lysine-coated suture was advanced about 17 mm intracranially from the common carotid artery bifurcation via the right and internal external carotid artery with halothane (0.5–1.5%) for 3 h[1].
Dosage: 20 mg/kg/h (loading infusion), 5 mg/kg/h (maintenance infusion)
Administration: i.v. infusion, loading infusion for 0.5 h followed by maintenance infusion from 2 or 3 h to 24 h after tMCA occlusion, and then measured infarct volume of ischemic damage.
Result: Significantly maintained neuroprotection even when given 2 h after the onset of ischemia in tMCA occlusion rat models, with the degree of protection against hemisphere and subcortical infarct volume by 34% and 37%, respectively.
Notably sustained the improvement of neurological deficit and the reduction of infarct volume (especially cortex by 39%) as well as increase of rat body weight for 1 week following the onset of ischemia in tMCA occlusion rat models.
分子量

414.56

Formula

C22H30N4O2S
CAS 号
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.
纯度 & 产品资料
参考文献

YM-202074 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

YM-202074299900-83-7YM202074YM 202074mGluRMetabotropic glutamate receptorsAntagonistmGluR1NeuroprotectionRat cerebellar granule cellsHEK cellsCHO cellstMCA occlusion rat modelInhibitorinhibitorinhibit

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