Sassolas G, Chatelain P, Cohen R, Boissel J P, Laporte S, Galleyrand J, Claustrat B, Elmcharfi A, Chayvialle J A, Cohen H
J Clin Endocrinol Metab. 1984 Oct;59(4):705-9. doi: 10.1210/jcem-59-4-705.
Synthetic human pancreatic tumor GH-releasing hormone (hpGRH 1-44-NH2) was given by iv bolus injection to 10 normal men at doses of 75, 150, 300, and 600 micrograms. At all doses the plasma GH responses were similar in an individual subject. Among subjects, however, the responses were significantly different, with peak GH concentrations ranging between 9.0 micrograms/liter and 54.9 micrograms/liter. The GH released in response to GRH was bioactive in the Nb2 lymphoma cell multiplication assay. The circulating GH 30 and 60 min after GRH was detected in 3 molecular forms corresponding to little, big, and big-big GH. These forms averaged 50%, 30%, and 20% of the total immunoreactive GH, respectively. The mean rise of plasma somatomedin-C, from 1.86 U/ml to 2.21 U/ml 24 h after GRH, was not statistically significant. A small but statistically significant GRH dose-dependent rise in plasma PRL (mean PRL concentrations 10 min after 600 micrograms GRH, 11.13 micrograms/liter occurred consistently after GRH injection. The evidence that the GH released by GRH is bioactive supports the potential use of GRH for therapeutic applications.
以静脉推注的方式,将合成的人胰腺肿瘤生长激素释放激素(hpGRH 1-44-NH2)以75、150、300和600微克的剂量给予10名正常男性。在所有剂量下,个体受试者的血浆生长激素反应相似。然而,在受试者之间,反应存在显著差异,生长激素峰值浓度在9.0微克/升至54.9微克/升之间。在Nb2淋巴瘤细胞增殖试验中,对生长激素释放激素作出反应而释放的生长激素具有生物活性。在生长激素释放激素给药后30分钟和60分钟检测到的循环生长激素有3种分子形式,分别对应小、大、大大生长激素。这些形式分别平均占总免疫反应性生长激素的50%、30%和20%。生长激素释放激素给药24小时后,血浆生长调节素-C的平均水平从1.86 U/ml升至2.21 U/ml,差异无统计学意义。生长激素释放激素注射后,血浆催乳素出现小幅度但具有统计学意义的剂量依赖性升高(600微克生长激素释放激素注射后10分钟的平均催乳素浓度为11.13微克/升)。生长激素释放激素释放的生长激素具有生物活性这一证据支持了生长激素释放激素在治疗应用中的潜在用途。