Rebuffé-Scrive M, Lundholm K, Björntorp P
Eur J Clin Invest. 1985 Oct;15(5):267-71. doi: 10.1111/j.1365-2362.1985.tb00182.x.
Binding of triamcinolone was examined in cytosolic preparations of human adipose tissue obtained during surgery. A saturable specific binding was found. Non-specific binding comprised on an average 28% of total binding. The affinity and concentration of binding sites were in the same order as previously described for glucocorticoid hormone binding in other tissues and in rat adipose tissue. There was a large difference in these variables between different individuals. The binding was inhibited competitively by non-labelled triamcinolone, promegestone, dexamethasone and 17-beta-estradiol, in that order of potency. The promegestone inhibition was effective requiring only about 25% higher concentration than triamcinolone to obtain inhibition of half the triamcinolone binding. There was more binding of triamcinolone in omental than in subcutaneous abdominal adipose tissue when expressed per unit of protein and per unit cell surface area but not when expressed per adipocyte.
在手术中获取的人脂肪组织的胞质制剂中检测了曲安奈德的结合情况。发现存在可饱和的特异性结合。非特异性结合平均占总结合的28%。结合位点的亲和力和浓度与先前在其他组织和大鼠脂肪组织中描述的糖皮质激素激素结合情况处于同一水平。不同个体之间这些变量存在很大差异。未标记的曲安奈德、普美孕酮、地塞米松和17-β-雌二醇按效力顺序竞争性抑制该结合。普美孕酮抑制有效,仅需比曲安奈德高约25%的浓度即可抑制一半的曲安奈德结合。以每单位蛋白质和每单位细胞表面积表示时,曲安奈德在网膜脂肪组织中的结合比皮下腹部脂肪组织中的更多,但以每个脂肪细胞表示时则不然。