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CAS No.: 1138245-13-2

Mirogabalin Catalog No. CSN19022

Synonyms: DS5565;A-2000700

Mirogabalin is a preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.

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技术信息

生物活性

描述Mirogabalin, a novel ligand for the α2δ subunit of voltage-gated calcium channels, is being developed to treat pain associated with diabetic peripheral neuropathy and postherpetic neuralgia. Mirogabalin shows potent and selective binding affinities for the human and rat α2δ subunits, and slower dissociation rates for the α2δ-1 subunit than the α2δ-2 subunit. It shows potent and long-lasting analgesic effects in rat models of neuropathic pain, and wider safety margins for side effects of the central nervous system^[3]. In rats subjected to spinal cord injury, mechanical allodynia was demonstrated by a decreased paw withdrawal threshold. A single oral administration of mirogabalin (2.5, 5, or 10 mg/kg) significantly increased the paw withdrawal threshold. The effects of mirogabalin were still significant 6 or 8 h after administration. The paw withdrawal threshold AUC was significantly higher in the treated animals than in the control group^[4]. Mirogabalin relieved DPNP (diabetic peripheral neuropathic pain) in a dose-dependent manner; mirogabalin 30 mg/day showed statistically significant pain relief (vs placebo) in Asian DPNP patients. All doses of mirogabalin tested were well tolerated^[5]. The most frequent treatment-emergent adverse events (TEAEs)-dizziness and somnolence-were expected based on mirogabalin's mechanism of action. After oral administration, mirogabalin was rapidly absorbed (time to maximum concentration, ∼1 hour) and eliminated through urine unchanged (61%-72% urinary excretion)^[6].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01496365	Diabetic Peripheral Neuropathy	Phase 2	Completed	-	-
NCT02187471	Pain Associated With Fibromyal... more >>gia Collapse <<	Phase 3	Completed	-	-
NCT02146430	Pain Associated With Fibromyal... more >>gia Collapse <<	Phase 3	Completed	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.7782 mL
- 23.8909 mL
- 47.7818 mL
- 5 mM
- 0.9556 mL
- 4.7782 mL
- 9.5564 mL
- 10 mM
- 0.4778 mL
- 2.3891 mL
- 4.7782 mL

技术信息

CAS号

1138245-13-2

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H19NO2

运输

蓝冰

分子量

209.28

别名

DS5565;A-2000700

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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Mirogabalin Catalog No. CSN19022

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