Knepel W, Homolka L, Vlaskovska M, Nutto D
Neuroendocrinology. 1984 May;38(5):344-50. doi: 10.1159/000123915.
Vasopressin analogs, which markedly differed in the ratio of pressor versus antidiuretic activity and also in ACTH/beta-endorphin-releasing activity, were used in the present study. The ability of vasopressin and these analogs to enhance the release of adrenocorticotropin-(ACTH-IR) and beta-endorphin-like immunoreactivity (beta-EI) induced by synthetic ovine corticotropin-releasing factor -CRF-(1-41)- was studied in vitro using incubated rat anterior pituitary quarters. Arginine vasopressin (AVP) potentiated the action of CRF-(1-41) 2- to 4-fold. Vasopressin analogs, which possess direct CRF-like activity when given alone, also enhanced beta-EI release caused by CRF-(1-41); the lowest concentration able to potentiate CRF-(1-41) activity was closely correlated with the ED50 value of these analogs for direct CRF-like activity. The vasopressin analog 1-(beta-mercapto-beta,beta-cyclopentamethylenepropionic acid)-2-(O-methyl)tyrosine-8-arginine-vasopressin blocked the release of ACTH-IR induced by AVP; however, this analog failed to prevent the potentiation by AVP of ACTH-IR release caused by CRF-(1-41), but enhanced itself the action of CRF-(1-41). Two analogs, which exhibited no direct CRF-like activity and which also did not antagonize the CRF-like activity of AVP, markedly enhanced the ACTH-IR and beta-EI response to CRF-(1-41).(ABSTRACT TRUNCATED AT 250 WORDS)
本研究使用了血管加压素类似物,它们在升压活性与抗利尿活性的比例以及促肾上腺皮质激素/β-内啡肽释放活性方面存在显著差异。使用孵育的大鼠垂体前叶片段在体外研究了血管加压素及其类似物增强由合成羊促肾上腺皮质激素释放因子-CRF-(1-41)-诱导的促肾上腺皮质激素(ACTH-IR)和β-内啡肽样免疫反应性(β-EI)释放的能力。精氨酸血管加压素(AVP)使CRF-(1-41)的作用增强了2至4倍。单独给药时具有直接CRF样活性的血管加压素类似物也增强了CRF-(1-41)引起的β-EI释放;能够增强CRF-(1-41)活性的最低浓度与这些类似物直接CRF样活性的ED50值密切相关。血管加压素类似物1-(β-巯基-β,β-环戊亚甲基丙酸)-2-(O-甲基)酪氨酸-8-精氨酸血管加压素阻断了AVP诱导的ACTH-IR释放;然而,该类似物未能阻止AVP对CRF-(1-41)引起的ACTH-IR释放的增强作用,但自身增强了CRF-(1-41)的作用。两种既无直接CRF样活性也不拮抗AVP的CRF样活性的类似物显著增强了对CRF-(1-41)的ACTH-IR和β-EI反应。(摘要截选至250字)