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编 号：F146900
分子式：C19H27NO3
分子量：317.42
分子式：C19H27NO3
分子量：317.42
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CAS No: 138847-85-5
产品详情
生物活性：
PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.
体内研究：
PRE-084 (0.25 mg/kg; i.p.; 3 times a week for 8 weeks) displays beneficial effects on motor performance (improves motor neuron survival, ameliorates paw abnormality and grip strength performance) in wobbler mice, and shows neuroprotective effects (increases the levels of BDNF in the gray matter).PRE-084 (1 mg/kg; i.p.; single) protects the heart by activating the Akt?eNOS pathway in myocardial infarction model.Animal Model:Wobbler mice (4-week-old).
Dosage:0.25 mg/kg
Administration:Intraperitoneal injection; 3 times a week for 8 weeks.
Result:Significantly improved ameliorated paw abnormality from week 4, and notably improved paw grip strength at week 5.Reduced the number of reactive astrocytes whereas increased the number of pan-macrophage marker CD68-positive cells and CD206+ cells involved in tissue restoration.Showed 26.5% increase in the mean number of large-size NISSL-positive motor neurons.
Animal Model:Adult male Sprague?Dawley rats (220-250 g; myocardial infarction model).
Dosage:1 mg/kg
Administration:Intraperitoneal injection; single.
Result:Significantly decreased the degree of myocardial apoptosis.Led to significantly increased expression of p?Akt and p?eNOS.
体外研究：
PRE-084 (0.1-100 μM; 24 h) protects cultured cortical neurons against β-amyloid toxicity (maximally neuroprotective at 10 μM) and reduces the levels of proapoptotic protein Bax at 10 μM.
PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.
体内研究：
PRE-084 (0.25 mg/kg; i.p.; 3 times a week for 8 weeks) displays beneficial effects on motor performance (improves motor neuron survival, ameliorates paw abnormality and grip strength performance) in wobbler mice, and shows neuroprotective effects (increases the levels of BDNF in the gray matter).PRE-084 (1 mg/kg; i.p.; single) protects the heart by activating the Akt?eNOS pathway in myocardial infarction model.Animal Model:Wobbler mice (4-week-old).
Dosage:0.25 mg/kg
Administration:Intraperitoneal injection; 3 times a week for 8 weeks.
Result:Significantly improved ameliorated paw abnormality from week 4, and notably improved paw grip strength at week 5.Reduced the number of reactive astrocytes whereas increased the number of pan-macrophage marker CD68-positive cells and CD206+ cells involved in tissue restoration.Showed 26.5% increase in the mean number of large-size NISSL-positive motor neurons.
Animal Model:Adult male Sprague?Dawley rats (220-250 g; myocardial infarction model).
Dosage:1 mg/kg
Administration:Intraperitoneal injection; single.
Result:Significantly decreased the degree of myocardial apoptosis.Led to significantly increased expression of p?Akt and p?eNOS.
体外研究：
PRE-084 (0.1-100 μM; 24 h) protects cultured cortical neurons against β-amyloid toxicity (maximally neuroprotective at 10 μM) and reduces the levels of proapoptotic protein Bax at 10 μM.
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