产品
编 号：F743638
分子式：C18H19ClFN3O2
分子量：363.81
分子式：C18H19ClFN3O2
分子量：363.81
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CAS No: 1261171-52-1
产品详情
生物活性：
mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments.
体外研究：
mGluR5 modulator 1 (compound 2c; 0.1-0.00001 nM) potentiates the L-glutamate and DHPG responses to the same maximum response as the orthosteric agonists alone in the Ca2+ mobilization and IP1 accumulation assays.mGluR5 modulator 1 (0.1-0.00001 nM) potentiates the L-glutamate and DHPG responses above the orthosteric agonist maximal response in the ERK1/2 phosphorylation assay.mGluR5 modulator 1 induces mGlu5 internalization in the absence of add orthosteric agonist or antagonist.mGluR5 modulator 1 potentiates the responses induced by both orthosteric agonists (L-glutamate or DHPG) in Ca2+ mobilization (pKB=5.4 and 5.3, respecyively), inositol monophosphate accumulation, and ERK1/2 phosphorylation signaling (pKB=5.88 and 5.4, respecyively) assays in HEK293A-mGlu5-low cells.mGluR5 modulator 1 enhances the effect of DHPG in cortical neurons with pEC50 values of 6.32 and 6.33 in Ca2+ mobilization andinositol monophosphate (IP1) accumulation assays.
mGluR5 modulator 1 is a mGluR5 positive allosteric modulator. mGluR5 modulator 1 can be used for the research of the schizophrenia and cognitive impairments.
体外研究：
mGluR5 modulator 1 (compound 2c; 0.1-0.00001 nM) potentiates the L-glutamate and DHPG responses to the same maximum response as the orthosteric agonists alone in the Ca2+ mobilization and IP1 accumulation assays.mGluR5 modulator 1 (0.1-0.00001 nM) potentiates the L-glutamate and DHPG responses above the orthosteric agonist maximal response in the ERK1/2 phosphorylation assay.mGluR5 modulator 1 induces mGlu5 internalization in the absence of add orthosteric agonist or antagonist.mGluR5 modulator 1 potentiates the responses induced by both orthosteric agonists (L-glutamate or DHPG) in Ca2+ mobilization (pKB=5.4 and 5.3, respecyively), inositol monophosphate accumulation, and ERK1/2 phosphorylation signaling (pKB=5.88 and 5.4, respecyively) assays in HEK293A-mGlu5-low cells.mGluR5 modulator 1 enhances the effect of DHPG in cortical neurons with pEC50 values of 6.32 and 6.33 in Ca2+ mobilization andinositol monophosphate (IP1) accumulation assays.
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