CGS 15435
CGS 15435 用途与合成方法
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TXA 2 1 nM (IC 50 ) |
CGS 15435 is a highly specific Tx synthetase inhibitor. CGS 15435 is only weakly effective as an inhibitor of PGE 2 (Cyclooxygenase, IC 50 =1200 μM), prostacyclin (PGI 2 synthetase, IC 50 =90 μM) or 5-Lipoxygenase (IC 50 =60 μM) product formation.
CGS 15435 has a long duration of action, since the increases in the plasma levels of TxB 2 are prevented even at 24 h after CGS 15435 administration. CGS 15435 significantly inhibits TxB 2 formation 4, 6, 12 and 24 h after dosing. Administration of CGS 15435 0.25 or 24 h prior to Arachidonic acid (AA) produced no increase in TxB 2 in the surviving animals (4/4 and 5/6, respectively). The final TxB 2 levels in the CGS15435A (0.25 and 24 h pretreatment) groups are significantly lower (P<0.05) than those seen in the AA or the Dazoxiben (2 h pretreatment) groups.
