产品
编 号：F624022
分子式：C15H16ClF2NO5S
分子量：395.81
分子式：C15H16ClF2NO5S
分子量：395.81
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1377615-44-5
产品详情
生物活性：
LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo.
体内研究：
LY3020371 hydrochloride (LY3020371.HCl) (Intravenous injection; 3-15 mg/kg)in rats leads to cerebrospinal fluid drug levels that are expected to effectively block mGlu2/3receptors.LY3020371 hydrochloride (LY3020371) (intraperitoneal injection; 3 mg/kg, 10?mg/kg; 2 hours) has clear wake promoting effects, resulting in a large reduction in NREM sleep in the Wistar rats during the light phase.
体外研究：
LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity (hmGlu2 Ki=5.26 nM; hmGlu3 Ki=2.50 nM).LY3020371 hydrochloride (LY3020371.HCl) (0.1 nM-100 μM; 1 hours) potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation (IC50=16.2 nM), an effect that was similarly observed in hmGlu3-expressing cells ( IC50=6.21 nM).LY3020371 hydrochloride (LY3020371.HCl)blocks agonist-suppressed spontaneous Ca2+ oscillations (IC50=34 nM) and in an intact hippocampal slice preparation (IC50=46 nM).
LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM. LY3020371 hydrochloride exerts an antidepressant-like signature in vivo.
体内研究：
LY3020371 hydrochloride (LY3020371.HCl) (Intravenous injection; 3-15 mg/kg)in rats leads to cerebrospinal fluid drug levels that are expected to effectively block mGlu2/3receptors.LY3020371 hydrochloride (LY3020371) (intraperitoneal injection; 3 mg/kg, 10?mg/kg; 2 hours) has clear wake promoting effects, resulting in a large reduction in NREM sleep in the Wistar rats during the light phase.
体外研究：
LY3020371 hydrochloride (LY3020371.HCl) displaces binding of the mGlu2/3 agonist ligand [3H]-459477 with high affinity (hmGlu2 Ki=5.26 nM; hmGlu3 Ki=2.50 nM).LY3020371 hydrochloride (LY3020371.HCl) (0.1 nM-100 μM; 1 hours) potently blocks mGlu2/3 agonist (DCG-IV)-inhibited, forskolin-stimulated cAMP formation (IC50=16.2 nM), an effect that was similarly observed in hmGlu3-expressing cells ( IC50=6.21 nM).LY3020371 hydrochloride (LY3020371.HCl)blocks agonist-suppressed spontaneous Ca2+ oscillations (IC50=34 nM) and in an intact hippocampal slice preparation (IC50=46 nM).
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