兽医药理学皮质激素系统药理_培训课件.pptVIP

江苏农牧科技职业学院 PDF created with pdfFactory Pro trial version 江苏农牧科技职业学院 PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version 外 用 醋酸肤轻松 PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version 肾上腺皮质激素的基本结构为甾核，构效关系非常密切： ① C3的酮基、C20的羰基及C4-5的双键是保持生理功能所必 需； ② 糖皮质激素的C17上有-OH；C11上有=O或-OH； ③ 盐皮质激素的C17上无-OH；C11上无=O或有O与C18相联； ④ C1-2为双键（泼尼松、氢化泼尼松）以及C6引入-CH3（甲氢 强的松）则抗炎作用增强、水盐代谢作用减弱； ⑤ C9引入-F（氢氟可的松），C16引入-CH3或-OH（去炎松） 则抗炎作用更强、水盐代谢作用更弱。 21 C H2O H 20 18 C 17 O 16 15 R 11 1 2 3 10 9 8 12 13 C A 4 5 D 14 B 6 7 O PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version HSP70 R HSP90 IPIP S S S R （不稳定） IPIP IPIP S R* S R* 激素-受体 二聚体（激活） DNA GRE S CBG 生物效应 功能蛋白 mRNA 编辑 细胞浆 S S S R* R* pre- mRNA 细胞核 ）） 转录复合体 （RNA聚合酶等） 糖皮质激素（GCS）基本作用模式 CBG：皮质激素转运球蛋白；S：糖皮质激素 ；R：糖皮质激素受体；R*：激 活的糖皮质激素受体； HSP：热休克蛋白；IP：免疫亲和素 PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version PDF created with pdfFactory Pro trial version 下丘脑 – – 长 负 反 馈 CRF ++ 垂体前叶 ACTH – 短 负 反 馈 – + 肾上腺