Matsukura S, Higashino H, Sakamoto N, Hirata Y, Imura H
Endocrinol Jpn. 1976 Apr;23(2):91-5. doi: 10.1507/endocrj1954.23.91.
The andrenocorticotrophic effect of a synthetic substituted adrenocorticortophic hormone (ACTH), alpha-1-18NH2-D-Ser1-Lys17, 18-ACTH (CIBA 47, 795-Ba) has been compared with that of alpha1-24-ACTH (tetracosactide), alpha1-24-ACTH depot (tetracosactide depot) and alpha1-18NH2-Gly1-ACTH (giractide) in the rabbit. Plasma corticosteroid levels after salin injection were higher in the afternoon than in the morning. The highest value was observed at 3 p.m. 41,795-Ba, either given intravenously or intramuscularly, was shown to be the most potent peptide followed by tetrocosactide depot and was 15 times more potent than tetracosactide and giractide in steroidogenic activity in the rabbit. The intravenous administration of 41,795-Ba caused more sustained stimulation of the adrenal cortex than the intramuscular injection. These results reveal the diurnal variation pattern of the pitutitary-adrenal axis of the rabbit similar to that of the rat and also confirm the finding that alpha1-18NH2-Dser1-Lys17, 18-ACTH is a potent adrenocorticotrophic peptide without the addition of any agent to delay its absorption in the rabbit.
已将一种合成的取代促肾上腺皮质激素（促肾上腺皮质激素），α-1-18NH₂-D-丝氨酸¹-赖氨酸¹⁷，18-促肾上腺皮质激素（CIBA 47,795-Ba）与α1-24-促肾上腺皮质激素（二十四肽促皮质素）、α1-24-促肾上腺皮质激素长效制剂（二十四肽促皮质素长效制剂）和α1-18NH₂-甘氨酸¹-促肾上腺皮质激素（吉拉肽）在兔体内的促肾上腺皮质作用进行了比较。注射生理盐水后，血浆皮质类固醇水平下午高于上午。最高值在下午3点观察到。41,795-Ba无论是静脉注射还是肌肉注射，都是最有效的肽，其次是二十四肽促皮质素长效制剂，其在兔体内的类固醇生成活性比二十四肽促皮质素和吉拉肽强15倍。静脉注射41,795-Ba比肌肉注射对肾上腺皮质的刺激更持久。这些结果揭示了兔垂体-肾上腺轴的昼夜变化模式与大鼠相似，也证实了α1-18NH₂-D-丝氨酸¹-赖氨酸¹⁷，18-促肾上腺皮质激素在兔体内是一种有效的促肾上腺皮质肽，无需添加任何延缓其吸收的药物。
