产品
编 号：F165628
分子式：C14H16Cl2N2O2
分子量：315.2
分子式：C14H16Cl2N2O2
分子量：315.2
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1445605-23-1
产品详情
生物活性：
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
体内研究：
Lu AF21934 treatment shows a dose-dependent anxiolytic-like effect in the stress-induced hyperthermia, four-plate, and marble-burying tests. The anti-hyperthermic effect of Lu AF21934 (5 mg/kg) in the SIH test is inhibited by the benzodiazepine receptor antagonist flumazenil (10 mg/kg) and is not serotonin dependent. Lu AF21934 does not produce antidepressant-like effects in the tail suspension test in mice; however, it decreases the basal locomotor activity of mice that are not habituated to activity cages. Lu AF21934 (0.5-5 mg/kg sc) does not influence tremor but at doses of 0.5 and 2.5 mg/kg reverses harmaline-induced hyperactivity. Lu AF21934 at a dose of 2.5 mg/kg potentiates the inhibitory influence of harmaline on the exploratory activity and AP1 during the first 30 min of the measurement and counteracts the harmaline-increased basic activity during the period of 30-90 min. Lu AF21934 (0.1-5 mg/kg) dose-dependently inhibits hyperactivity induced by MK-801 or amphetamine. It also antagonizes head twitches and increases frequency of spontaneous excitatory postsynaptic currents in brain slices, induced by DOI.
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
体内研究：
Lu AF21934 treatment shows a dose-dependent anxiolytic-like effect in the stress-induced hyperthermia, four-plate, and marble-burying tests. The anti-hyperthermic effect of Lu AF21934 (5 mg/kg) in the SIH test is inhibited by the benzodiazepine receptor antagonist flumazenil (10 mg/kg) and is not serotonin dependent. Lu AF21934 does not produce antidepressant-like effects in the tail suspension test in mice; however, it decreases the basal locomotor activity of mice that are not habituated to activity cages. Lu AF21934 (0.5-5 mg/kg sc) does not influence tremor but at doses of 0.5 and 2.5 mg/kg reverses harmaline-induced hyperactivity. Lu AF21934 at a dose of 2.5 mg/kg potentiates the inhibitory influence of harmaline on the exploratory activity and AP1 during the first 30 min of the measurement and counteracts the harmaline-increased basic activity during the period of 30-90 min. Lu AF21934 (0.1-5 mg/kg) dose-dependently inhibits hyperactivity induced by MK-801 or amphetamine. It also antagonizes head twitches and increases frequency of spontaneous excitatory postsynaptic currents in brain slices, induced by DOI.
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