产品
编 号：F624021
分子式：C15H15F2NO5S
分子量：359.35
分子式：C15H15F2NO5S
分子量：359.35
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CAS No: 1377615-75-2
产品详情
生物活性：
LY3020371 is a potent and selective antagonist of glutamate (mGlu) 2/3 receptor, with Kis of 5.26 and 2.50 nM for hmGluR2 and hmGluR3, respectively. LY3020371 can be used for the research of depression.
体内研究：
LY3020371 (0.3-3 mg/kg, a single i.v.) significantly increases the number of spontaneously active dopamine cells in the ventral tegmental area (VTA) of rats.LY3020371 (1-10 mg/kg, i.p. once a week for 5 weeks) dose dependently increases tissue oxygen in the anterior cingulate cortex (ACC) of rats.LY3020371 (10 mg/kg, a single i.p.) increases in monoamine efflux in the medial prefrontal cortex of freely moving rats.LY3020371 (1-30 mg/kg, a single i.v.) increases the cumulative wake time of rats in a dose- and time-dependent manner without rebound hypersomnolence.LY3020371 (0.1-10 mg/kg, a single i.v.) decrease the time rats are immobile in the forced-swim test in the rat forced-swim assay.Animal Model:Male Sprague-Dawley rats (230-350 g)
Dosage:0.3, 1, 3 mg/kg
Administration:I.v. daily 5 days per week for 2 weeks
Result:Increased the number of actively firing dopamine neurons in the VTA of anesthetized rats.
体外研究：
LY3020371 (0.1 nM-100 μM) competitively displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity.LY3020371 (0.1 nM-100 μM) blocks DCG-IV-induced inhibition of forskolin-stimulated cAMP production in cells expressing recombinant human mGlu2 (IC50=16.2 nM) and mGlu3 (IC50=6.21 nM) receptors.LY3020371 (0.3-30000 nM) exhibits concentration-dependent antagonism of LY379268-inhibited cAMP formation.LY3020371 (1-10000 nM) reverses LY379268-suppressed, K+-evoked glutamate release, with an IC50 of 86 nM.LY3020371 (0.3-10000 nM) leads to a concentration-dependent and complete blockade of the LY379268-suppressed response, with an IC50 of 33.9 nM.
LY3020371 is a potent and selective antagonist of glutamate (mGlu) 2/3 receptor, with Kis of 5.26 and 2.50 nM for hmGluR2 and hmGluR3, respectively. LY3020371 can be used for the research of depression.
体内研究：
LY3020371 (0.3-3 mg/kg, a single i.v.) significantly increases the number of spontaneously active dopamine cells in the ventral tegmental area (VTA) of rats.LY3020371 (1-10 mg/kg, i.p. once a week for 5 weeks) dose dependently increases tissue oxygen in the anterior cingulate cortex (ACC) of rats.LY3020371 (10 mg/kg, a single i.p.) increases in monoamine efflux in the medial prefrontal cortex of freely moving rats.LY3020371 (1-30 mg/kg, a single i.v.) increases the cumulative wake time of rats in a dose- and time-dependent manner without rebound hypersomnolence.LY3020371 (0.1-10 mg/kg, a single i.v.) decrease the time rats are immobile in the forced-swim test in the rat forced-swim assay.Animal Model:Male Sprague-Dawley rats (230-350 g)
Dosage:0.3, 1, 3 mg/kg
Administration:I.v. daily 5 days per week for 2 weeks
Result:Increased the number of actively firing dopamine neurons in the VTA of anesthetized rats.
体外研究：
LY3020371 (0.1 nM-100 μM) competitively displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity.LY3020371 (0.1 nM-100 μM) blocks DCG-IV-induced inhibition of forskolin-stimulated cAMP production in cells expressing recombinant human mGlu2 (IC50=16.2 nM) and mGlu3 (IC50=6.21 nM) receptors.LY3020371 (0.3-30000 nM) exhibits concentration-dependent antagonism of LY379268-inhibited cAMP formation.LY3020371 (1-10000 nM) reverses LY379268-suppressed, K+-evoked glutamate release, with an IC50 of 86 nM.LY3020371 (0.3-10000 nM) leads to a concentration-dependent and complete blockade of the LY379268-suppressed response, with an IC50 of 33.9 nM.
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