Keenan J, Thompson J B, Chamberlain M A, Besser G M
Br Med J. 1971 Sep 25;3(5777):742-3. doi: 10.1136/bmj.3.5777.742.
The adrenocorticotrophic effects of a synthetic corticotrophin analogue, alpha(1-18) ACTH with D-serine(1), lysine(17), and lysine amide(18) substitutions has been studied. It is effective after both intramuscular and subcutaneous administration and compared with tetracosactrin depot (Synacthen depot, Cortrosyn depot) it has a similarly prolonged time course of action-about 24 hours after 0.5 mg and 30 hours after 1 mg. Unlike tetracosactrin depot, however, it is well absorbed when given intranasally and does not produce painful reactions at the site of injection. Its prolonged time course of action does not depend on a formulation designed to delay its release from the injection site but most probably on a decreased rate of degradation in the circulation.
已对一种合成促肾上腺皮质激素类似物α(1 - 18)促肾上腺皮质激素(ACTH)进行了研究,该类似物具有D - 丝氨酸(1)、赖氨酸(17)和赖氨酸酰胺(18)取代基。肌内和皮下给药后均有效,与长效二十四肽促皮质素(长效合成促皮质素、长效考的松)相比,其作用时间进程相似——0.5毫克后约24小时,1毫克后约30小时。然而,与长效二十四肽促皮质素不同,经鼻给药时它吸收良好,且在注射部位不会产生疼痛反应。其延长的作用时间进程并非取决于旨在延缓其从注射部位释放的制剂,而很可能取决于循环中降解速率的降低。