产品
编 号:F234803
分子式:C24H30N4O3
分子量:422.52
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10mM*1mL in DMSO
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1mg
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5mg
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生物活性:
PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy.

体内研究:
PNU-142633 (0.03-1 mg/kg; intravenous injection; male Hartley guinea pigs) treatment blocks neurogenic plasma protein extravasation. And PNU-142633 fails to alter resistance in these vascular beds.Animal Model:Male Hartley guinea pigs (250-300 g) stimulated with bipolar electrode
Dosage:0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration:Intravenous injection
Result:Significantly reduced extravasation at the 0.1 and 0.3 mg/kg doses, but was without effect at the 0.03 and 1.0 mg/kg doses.

体外研究:
The intrinsic activity of PNU-142633 at the human 5-HT1D receptor is determined to be 70% that of 5-HT in a cytosensor cell-based assay compared with 84% for that of Sumatriptan.
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