Sassolas G, Biot-Laporte S, Cohen R, Chatelain P, Boissel J P, Dupin P, Garry P, Claustrat B, Girard P, Borson F
Horm Res. 1986;24(2-3):99-111. doi: 10.1159/000180548.
A dose-effect relationship between human growth hormone (GH) releasing factor (hGRF) and GH response was demonstrated for doses ranging from 5 micrograms per subject (minimal active dose) to 40-80 micrograms per subject (minimal dose for maximal effect). Bioactivity of GH released under hGRF was proven in the Nb2 lymphoma cell multiplication assay. Unwanted effects were observed for doses equal to or larger than 150 micrograms. Pharmacokinetic parameters were calculated from the immunoreactive GRF plasma concentrations obtained after intravenous injections of various doses. The half-lives were 6.8 +/- 0.4 min and 43.2 +/- 3 min for distribution and elimination phases, respectively. Subcutaneous administration of hGRF was shown to be effective for promoting GH release, with doses higher than those required by intravenous administration. Intermittent intravenous injection of hGRF, at 3-hour intervals, resulted in a decrease in the magnitude of GH response in normal subjects.
已证明，对于每受试者5微克（最小活性剂量）至每受试者40 - 80微克（最大效应的最小剂量）的剂量范围，人生长激素（GH）释放因子（hGRF）与GH反应之间存在剂量效应关系。在Nb2淋巴瘤细胞增殖试验中证实了hGRF作用下释放的GH的生物活性。对于等于或大于150微克的剂量，观察到了不良效应。根据静脉注射不同剂量后获得的免疫反应性GRF血浆浓度计算药代动力学参数。分布期和消除期的半衰期分别为6.8±0.4分钟和43.2±3分钟。皮下注射hGRF被证明对促进GH释放有效，所需剂量高于静脉注射所需剂量。正常受试者每隔3小时间歇性静脉注射hGRF会导致GH反应幅度降低。
