Adams E F, Ashby M J, Burrin J, Yeo T H, Drucker R, Stringer K, Mashiter K
Clin Endocrinol (Oxf). 1985 May;22(5):631-8. doi: 10.1111/j.1365-2265.1985.tb02999.x.
The effects of nivazol, a novel steroid which lacks glucocorticoid activity, on ACTH secretion by cell cultures of human pituitary corticotrophic tumours has been investigated. Nivazol (0.002-20 mumol/l) inhibited ACTH secretion by 50-80%, after 4 and 24 h of incubation. (Trilostane (0.3-30 mumol/l) did not affect basal or stimulated ACTH secretion.) The potency of nivazol was comparable with that of hydrocortisone, and less than dexamethasone. The stimulatory effects of oCRF and AVP were reduced or completely blocked by nivazol in a similar manner to that previously described for hydrocortisone. It is concluded that nivazol may be of benefit in the direct treatment of Cushing's disease, particularly since it lacks glucocorticoid activity.
已对一种缺乏糖皮质激素活性的新型类固醇尼伐唑对人垂体促肾上腺皮质激素肿瘤细胞培养物促肾上腺皮质激素(ACTH)分泌的影响进行了研究。在孵育4小时和24小时后,尼伐唑(0.002 - 20μmol/L)可使ACTH分泌减少50 - 80%。(曲洛司坦(0.3 - 30μmol/L)不影响基础或刺激后的ACTH分泌。)尼伐唑的效力与氢化可的松相当,且低于地塞米松。与先前描述的氢化可的松类似,尼伐唑以相似的方式降低或完全阻断了促肾上腺皮质激素释放因子(oCRF)和血管加压素(AVP)的刺激作用。得出的结论是,尼伐唑可能对库欣病的直接治疗有益,特别是因为它缺乏糖皮质激素活性。