产品
编 号：F247148
分子式：C19H27N3O2S
分子量：361.5
分子式：C19H27N3O2S
分子量：361.5
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1997387-43-5
产品详情
生物活性：
PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
体内研究：
PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. PZM21 is efficacious for the affective component of analgesia versus the reflexive component and is devoid of respiratory depression in mice at equi-analgesic doses. PZM21 displays dose-dependent analgesia in a mouse hotplate assay, with a per cent maximal possible effect (% MPE) of 87% reached 15 min after administration of the highest dose of drug tested .PZM21 has a long-lasting analgesic effect on CNS mediated-pain responses, but does not cause respiratory depression and constipation, two key side effects of opioid agonists.
体外研究：
PZM21 has no detectable κOR or nociceptin receptor agonist activity-it is actually an 18 nM κOR antagonist-while it is a 500-fold weaker δOR agonist, making it a selective μOR agonist.At hERG, PZM21 has an IC50 of between 2 and 4 μM, 500- to 1,000-fold weaker than its potency as a μOR agonist. Signalling by PZM21 and other μOR agonists appears to be mediated primarily by the heterotrimeric G protein Gi/o, as its effect on cAMP levels is eliminated by pertussis toxin and no activity is observed in a calcium release assay .
PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
体内研究：
PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. PZM21 is efficacious for the affective component of analgesia versus the reflexive component and is devoid of respiratory depression in mice at equi-analgesic doses. PZM21 displays dose-dependent analgesia in a mouse hotplate assay, with a per cent maximal possible effect (% MPE) of 87% reached 15 min after administration of the highest dose of drug tested .PZM21 has a long-lasting analgesic effect on CNS mediated-pain responses, but does not cause respiratory depression and constipation, two key side effects of opioid agonists.
体外研究：
PZM21 has no detectable κOR or nociceptin receptor agonist activity-it is actually an 18 nM κOR antagonist-while it is a 500-fold weaker δOR agonist, making it a selective μOR agonist.At hERG, PZM21 has an IC50 of between 2 and 4 μM, 500- to 1,000-fold weaker than its potency as a μOR agonist. Signalling by PZM21 and other μOR agonists appears to be mediated primarily by the heterotrimeric G protein Gi/o, as its effect on cAMP levels is eliminated by pertussis toxin and no activity is observed in a calcium release assay .
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