生物活性 | |||
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描述 | MK-677 is a potent, orally active growth hormone (GH) secretagogue with EC50 value of 1.3nM for releasing GH from rat pituitary cells in culture. Addition of 10nM MK-677 elicited transient elevations of cytosolic free calcium through the activation of L-type Ca2+ channels in rat somatotrophs. MK-677 at concentration of 0.1μM greatly potentiated the effect of GHRH (10nM) on GH release and the accumulation of intracellular cAMP in the pituitary cell assay. Elevation of GH could be observed in dogs after oral doses of MK-677 as low as 0.125mg/kg, without significant effect on plasma levels of aldosterone, luteinizing hormone, thyroxine, and prolactin after oral administration of 1 mg/kg. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.60mL 0.32mL 0.16mL |
8.00mL 1.60mL 0.80mL |
16.01mL 3.20mL 1.60mL |
参考文献 |
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