Pyridazines XVIII. 6-Aryl-3(2H)-Pyridazinones Inhibit Calcium Influx in Stimulated Platelets

概要

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6-Phenyl-5-hydroxymethyl-4,5-dihydro-3(2H)-pyridazinone (1) and 6-thienyl-5-hydroxymethyl-4,5-dihydro-3(2H)-pyridazinone (2) inhibit platelet aggregation induced by thrombin (IC_<50>=0.25 and 0.26 mM, respectively) or by the calcium ionophore ionomycin (IC<50>=0.42 and 0.43 mM, respectively). Pyridazinones 1 and 2 also show concentration-dependent attenuation of the increases in platelet cytosolic free calcium concentration induced by thrombin and ionomycin, suggesting that their antiaggregatory activity may be due to their capacity to inhibit the passage of calcium through the cytoplasmic membrane. This effect may be implicated in other pharmacological activities of 6-aryl-5-substituted-pyridazinones.
公益社団法人日本薬学会の論文
1999-12-15