Kripalani K J, Dean A V, Migdalof B H
Xenobiotica. 1983 Dec;13(12):701-5. doi: 10.3109/00498258309052231.
The metabolism of [14C]captopril-L-cysteine was studied in spontaneously hypertensive rats and pure-bred beagles after a single i.v. dose (4 mg/kg). During the first 24 h, concn. of total radioactivity in blood were similar in both species. Captopril was found in small amounts in the blood of both species. In rats, captopril, bound covalently but reversibly to plasma proteins (CP-PR), was the major component in blood (70%), whereas captopril-L-cysteine was a minor component (23%) of the total radioactivity. In dog blood, CP-PR constituted a smaller fraction (45%) of the total radioactivity than in the rat and captopril-L-cysteine was the major component (53%). In 72 h, 89-91% of the dose was excreted in the urine of rats and dogs. Captopril-L-cysteine accounted for 7% (rat) and 68% (dog) of the radioactivity in urine; captopril accounted for 75% (rat) and 7% (dog). Other metabolites were present in the urine of both species. The greater net conversion of captopril-L-cysteine to CP-PR and to captopril in rats helps explain why captopril-L-cysteine is excreted in urine as a major metabolite of captopril in dogs but only a minor one in rats.
在自发性高血压大鼠和纯种比格犬静脉注射单次剂量（4毫克/千克）[¹⁴C]卡托普利 - L - 半胱氨酸后，对其代谢情况进行了研究。在最初的24小时内，两种动物血液中总放射性浓度相似。在两种动物的血液中均发现了少量卡托普利。在大鼠中，与血浆蛋白共价结合但可逆结合的卡托普利（CP - PR）是血液中的主要成分（70%），而卡托普利 - L - 半胱氨酸是总放射性的次要成分（23%）。在犬类血液中，CP - PR在总放射性中所占比例（45%）低于大鼠，且卡托普利 - L - 半胱氨酸是主要成分（53%）。在72小时内，89 - 91%的剂量经大鼠和犬的尿液排出。卡托普利 - L - 半胱氨酸在大鼠尿液放射性中占7%，在犬尿液中占68%；卡托普利在大鼠尿液中占75%，在犬尿液中占7%。两种动物的尿液中均存在其他代谢产物。卡托普利 - L - 半胱氨酸在大鼠体内向CP - PR和卡托普利的净转化率更高，这有助于解释为什么卡托普利 - L - 半胱氨酸在犬尿液中作为卡托普利的主要代谢产物排出，而在大鼠尿液中只是次要代谢产物。
