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编 号:F744904
分子式:C50H72N12O9
分子量:985.18
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生物活性:
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity.

体内研究:
Intravenous administration of GR 83074 (Compound 10) to anaesthetized, artificially-respired guinea-pigs (0.3 μmol/kg) causes a marked antagonism of the increase in tracheal insufflation pressure induced by the NK-2 agonist, GR64349.

体外研究:
In the isolated rat colon and guinea-pig trachea, GR 83074 is a potent competitive antagonist of the contractions induced by the selective NK-2 agonist GR6434.
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