Abdulkader R C, Silva H B, Marcondes M, Vasconcelos E A, Paiva A C
J Pharm Pharmacol. 1979 Jan;31(1):20-2. doi: 10.1111/j.2042-7158.1979.tb13414.x.
Depot administration of a lipophilic angiotensin II (AII) antagonist was tested for obtaining prolonged inhibition of the pressor response to AII in rats. Intramuscular injections of 1.5 or 5.0 mg of octanoyl-[Leu8]AII (oct-LAII), in oil solution produced the same degree of AII inhibition either 6 h or 24 h after the injection. The inhibition was comparable to that expected from the continuous intravenous infusion of oct-LAII at the rate of 1.2 microgram kg-1 min-1. The prolonged effect of intramuscular injections of oct-LAII in oil solution may be useful for chronic studies of physiopathological states involving the renin-angiotensin-aldosterone system.
为了在大鼠中获得对血管紧张素II（AII）升压反应的长期抑制，对亲脂性AII拮抗剂进行了长效注射剂的测试。肌肉注射1.5或5.0毫克油溶液中的辛酰基-[亮氨酸8]AII（oct-LAII），在注射后6小时或24小时产生相同程度的AII抑制。这种抑制作用与以1.2微克/千克·分钟-1的速率持续静脉输注oct-LAII所预期的抑制作用相当。油溶液中肌肉注射oct-LAII的长效作用可能有助于涉及肾素-血管紧张素-醛固酮系统的生理病理状态的慢性研究。
