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卡托普利二硫化物二聚体(SQ 14,551)的缓激肽增强活性。

Bradykinin-potentiating activity of captopril disulphide dimer (SQ 14,551).

作者信息

Drummer O H, Kourtis S

机构信息

University of Melbourne, Department of Medicine, Austin Hospital, Heidelberg, Victoria, Australia.

出版信息

Eur J Pharmacol. 1988 Aug 9;153(1):11-7. doi: 10.1016/0014-2999(88)90582-1.

Abstract

The ability of captopril and one of its metabolites, the disulphide dimer have been studied for their ability to affect angiotensin I and bradykinin responses. Captopril disulphide dimer (i.v.) potentiated the vasodilatory effects of bradykinin in urethane-anaesthetized rats, at doses of 0.1 and 0.3 mg/kg but did not inhibit the angiotensin I-mediated pressor response at these same concentrations. This activity of captopril disulphide dimer in vivo was not seen with bradykinin responses in isolated guinea pig ileum except at bath concentrations much higher than for captopril (10(-5) M). However captopril and captopril disulphide dimer at oral doses of 10 mg/kg both lowered systolic and diastolic blood pressures in spontaneously hypertensive rats. These studies are consistent with an in vivo bradykinin-potentiating activity of captopril disulphide dimer and suggest a possible antihypertensive activity of disulphide metabolites of captopril.

摘要

已经研究了卡托普利及其一种代谢产物二硫化物二聚体影响血管紧张素I和缓激肽反应的能力。卡托普利二硫化物二聚体(静脉注射)在0.1和0.3mg/kg剂量下可增强缓激肽在氨基甲酸乙酯麻醉大鼠中的血管舒张作用,但在相同浓度下不抑制血管紧张素I介导的升压反应。除了在比卡托普利高得多的浴液浓度(10(-5)M)下,卡托普利二硫化物二聚体在体内的这种活性在离体豚鼠回肠的缓激肽反应中未观察到。然而,口服剂量为10mg/kg的卡托普利和卡托普利二硫化物二聚体均可降低自发性高血压大鼠的收缩压和舒张压。这些研究与卡托普利二硫化物二聚体在体内的缓激肽增强活性一致,并提示卡托普利二硫化物代谢产物可能具有抗高血压活性。

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