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编 号:F088996
分子式:C15H21N5O5
分子量:351.36
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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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生物活性:
GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions.

体内研究:
GR79236 decreases locomotor activity and inhibits DMCM-induced seizures in mice (ED50s of 0.13 mg/kg and 0.3 mg/kg, respectively). Oral administration of GR79236 (0.1-10 mg/kg) to fed rats induces minimal changes in the plasma concentration of non-esterified fatty acids and in the blood concentrations of glucose and lactate. Intravenous infusion of GR79236 to fasted pithed rats, or oral administration of GR79236 to fasted conscious rats and dogs, produces time- and dose-dependent decreases in the plasma non-esterified fatty acid concentration. In the fasted rats, doses of GR79236 that lowered plasma levels of non-esterified fatty acids also produced hypotriglyceridaemia and anti-ketotic effects.

体外研究:
GR79236 inhibits Isoprenaline-stimulated cAMP accumulation in DDT-MF2 cells with an IC50 of 2.6 nM. GR79236 inhibits catecholamine-induced lipolysis in human, rat and dog isolated adipocytes.
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