Blake J, Li C H
J Med Chem. 1976 Oct;19(10):1252-4. doi: 10.1021/jm00232a017.
An adrenocorticotropin analogue, [2-delta-aminovaleric acid, 5-arginine]adrenocorticotropin-(2-19), has been synthesized by the solid-phase method and its biological activity has been determined. It was found that substitution of arginine for glutamic acid at position 5 of [2-delta-aminovaleric acid]adrenocorticotropin-(2-19) increased the steroidogenic potency in idolated rat adrenal cells and the lipolytic potency in isolated rat fat cells but decreased the lipolytic potency in isolated rabbit fat cells. The synthetic analogue had only 2% of the melanotropic potency of the parent molecule.
一种促肾上腺皮质激素类似物，即[2-δ-氨基戊酸，5-精氨酸]促肾上腺皮质激素-(2-19)，已通过固相法合成，并测定了其生物活性。结果发现，在[2-δ-氨基戊酸]促肾上腺皮质激素-(2-19)的第5位用精氨酸取代谷氨酸，可提高离体大鼠肾上腺细胞的类固醇生成能力和离体大鼠脂肪细胞的脂解能力，但会降低离体兔脂肪细胞的脂解能力。该合成类似物的促黑素细胞活性仅为母体分子的2%。
