AMINO METHYL CYCLOHEXANE CARBOXYLIC ACID (AMCHA) A NEW SYNTHETIC FIBRINOLYTIC INHIBITOR
AMINO METHYL CYCLOHEXANE CARBOXYLIC ACID (AMCHA) A NEW SYNTHETIC FIBRINOLYTIC INHIBITOR
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DOI：
10.1111/j.1365-2141.1965.tb06583.x
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发表时间：
1965-01-01
影响因子：
6.5
通讯作者：
DOUGLAS, AS
中科院分区：
文献类型：
--
作者：
DUBBER, AHC;MCNICOL, GP;DOUGLAS, AS
合成的氨基酸，氨基甲基环己烷羧酸（AMCHA），在其立体异构体的天然存在的混合物的形式进行了研究。当浓度高于10-4 [image]时，异构体的混合物是纤溶酶原激活的竞争性抑制剂，而当浓度高于10-2 [image]时，是纤溶酶的非竞争性抑制剂。AMCHA竞争性抑制肠激酶对胰蛋白酶原的激活，但在4倍浓度下非竞争性抑制胰蛋白酶的蛋白水解活性。AMCHA抑制胃蛋白酶的蛋白水解活性。AMCHA制剂的研究有2倍的增益在体内的效力相比，N-氨基己酸（EACA），目前可用的纤溶抑制剂。
The synthetic amino acid, amino methyl cyclohexane carboxylic acid (AMCHA), was studied in the form of the naturally occurring mixture of its stereospecific isomers. At concentrations above 10-4 [image], the mixture of isomers is a competitive inhibitor of plasminogen activation, and at concentrations above 10-2 [image] is an uncompetitive inhibitor of plasmin. AMCHA competitively inhibits the activation of trypsinogen by enterokinase but non-competitively inhibits the proteolytic activity of trypsin at 4-fold greater concentrations. AMCHA inhibits the proteolytic activity of pepsin. The preparation of AMCHA investigated had in vivo a 2-fold gain in potency compared with epsilon amino caproic acid (EACA), the presently available fibrinolytic inhibitor.