Norquetiapine-d8 is a stable isotope labeled version of Norquetiapine, which acts as a selective inhibitor of HCN1 channels with an IC50 of 13.9 μM. This compound effectively inhibits noradrenaline reuptake and serves as a partial agonist at the 5-HT1A receptor (Ki = 45 nM), while also antagonizing presynaptic α2 (Ki = 237 nM), 5-HT2C (Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Furthermore, Norquetiapine exhibits state-dependent blockade of the human cardiac sodium channel Nav1.5 and demonstrates partial anti-inflammatory activity in LPS-injected C57BL/6 mice, making it useful for research on depression and inflammation.
Norquetiapine-d8 is a stable isotope labeled version of Norquetiapine, which acts as a selective inhibitor of HCN1 channels with an IC50 of 13.9 μM. This compound effectively inhibits noradrenaline reuptake and serves as a partial agonist at the 5-HT1A receptor (Ki = 45 nM), while also antagonizing presynaptic α2 (Ki = 237 nM), 5-HT2C (Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Furthermore, Norquetiapine exhibits state-dependent blockade of the human cardiac sodium channel Nav1.5 and demonstrates partial anti-inflammatory activity in LPS-injected C57BL/6 mice, making it useful for research on depression and inflammation.
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