LY2979165
产品说明书
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同义名 : | - |
| CAS号 : | 1311385-32-6 | |
| 货号 : | A198383 | |
| 分子式 : | C13H22N6O6S | |
| 纯度 : | 99%+ | |
| 分子量 : | 390.42 | |
| MDL号 : | MFCD25541740 | |
| 存储条件： |
Pure form Inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
H2O: 50 mg/mL(128.07 mM) |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Metabotropic glutamate (mGlu) receptors are Class C 7-transmembrane domain (7-TMD) G-protein coupled receptors (GPCRs) involved in the modulation of neurotransmission throughout the nervous system [3]. LY2979165 is the alanine prodrug of 2812223, a selective orthosteric mGluR2 agonist. It has been developed with the aim of normalizing aberrant glutamatergic activity in the human brain, and dose-dependently reversed ketamine-evoked increases in glucose metabolism in the rat brain as assayed by 2-deoxyglucose (2-DG) autoradiography [4]. LY2979165 would attenuate the ketamine-evoked BOLD (blood oxygenation level dependent) signal in a dose- and exposure-dependent fashion. A significant mean decrease of 45% in the ketamine-evoked signal at the 60-mg dose of LY2979165 compared to placebo, while the 20-mg dose showed an intermediate level of effect but no statistical separation from placebo. Additionally, pretreatment with LY2979165 dose-dependently augmented the ketamine-induced increases in the cognitive and positive subscales (PANSS), statistically significant (P = 0.008 and P = 0.005, respectively) at the 60-mg dose compared to placebo) [4]. | ||
| 作用机制 | LY2979165 is a mGlu2 agonist, a drug candidate drug used to treat bipolar disorder. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.56mL 0.51mL 0.26mL |
12.81mL 2.56mL 1.28mL |
25.61mL 5.12mL 2.56mL |
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