生物活性 | |||
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描述 | Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with Kis of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline (0.5-2 mM; 24-120 hours) treatment inhibits the proliferation of LNCaP-LN3 cells in a time- and dose-dependent manner. Pargyline (0.5-2 mM; 24-48 hours) treatment decreases S phase and increases the G1 phase in the cells in a dose-dependent manner. Pargyline (0.5 mM; 24 hours) treatment increases the apoptotic cells. Pargyline (2 mM; 48 hours treatment induces an increase of cytochrome c and a decrease of caspase-3 in the cells, but does not lead to a change of BCL-2 expression[2]. Pargyline (10 mg/kg; iv) treatment induces a moderate (about 20 mm Hg) but persistent (48 h) decrease of systolic blood pressure in unanesthetized adult spontaneously hypertensive rats (SHR) but not in normotensive rats. A low dose of Pargyline (200 μg; icv) injected directly into the brain lowered arterial pressure. The hypotensive action of Pargylline in SHR appears to be the consequence of Norepinephrine accumulating at an inhibitory α-adrenoceptor in brain[3]. Oral pargyline treatment protected transplanted beta cells in diabetic mice, thus leading to disease reversal. Furthermore, pargyline prevented or delayed diabetes onset in several mouse models for T1D(Type 1 diabetes)[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
6.28mL 1.26mL 0.63mL |
31.40mL 6.28mL 3.14mL |
62.80mL 12.56mL 6.28mL |
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