Nastorazepide (Z-360) hemicalcium is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide hemicalcium inhibits the specific binding of [ 3 H]CCK-8 to the human CCK-2 receptor with a K i value of 0.47 nM. Nastorazepide hemicalcium inhibits IL-1β , ephrin B1 , VEGF , and HIF-1alpha , reduces Akt and NR2B phosphorylation. Nastorazepide hemicalcium has antitumor activity against pancreatic cancer . Nastorazepide hemicalcium inhibits colorectal cancer liver metastasis and relieves pain.
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