Barron J L, Coy D H, Millar R P
Peptides. 1985 May-Jun;6(3):575-7. doi: 10.1016/0196-9781(85)90124-x.
Synthetic analogs of growth hormone-releasing hormone, GHRH(1-29)-NH2 and D-Ala2 GHRH(1-29)-NH2 were administered as a bolus intravenous injection to five normal men in a dose range of 0.015 to 0.5 micrograms/kg body weight. Vehicle only was administered in a control study. Peak responses to GHRH analogs occurred at 15 or 30 min. An increase in the integrated plasma growth hormone (GH) response was observed at each dose. The dose-response curve of GHRH(1-29)-NH2 indicated that it has a similar molar potency to GHRH(1-40) and GHRH(1-44). The potency of D-Ala2 GHRH(1-29)-NH2 was approximately twice that of GHRH(1-29)-NH2. Neither analog affected blood levels of PRL, TSH, LH, FSH, ACTH, insulin, glucagon, glucose, cortisol, free thyroxine, and free triiodothyronine. No side effects were noted other than transient flushing with the highest dose administered. The findings demonstrate GHRH(1-29)-NH2 and its D-Ala2 analog are potent stimulators of GH release and have potential application in clinical medicine.
将生长激素释放激素的合成类似物GHRH(1 - 29)-NH2和D - Ala2 GHRH(1 - 29)-NH2以0.015至0.5微克/千克体重的剂量范围静脉推注给药于5名正常男性。在对照研究中仅给予赋形剂。对GHRH类似物的峰值反应出现在15或30分钟。在每个剂量下均观察到血浆生长激素(GH)综合反应增加。GHRH(1 - 29)-NH2的剂量反应曲线表明其摩尔效力与GHRH(1 - 40)和GHRH(1 - 44)相似。D - Ala2 GHRH(1 - 29)-NH2的效力约为GHRH(1 - 29)-NH2的两倍。两种类似物均未影响PRL、TSH、LH、FSH、ACTH、胰岛素、胰高血糖素、葡萄糖、皮质醇、游离甲状腺素和游离三碘甲状腺原氨酸的血药浓度。除了给予最高剂量时出现短暂脸红外,未观察到其他副作用。这些发现表明GHRH(1 - 29)-NH2及其D - Ala2类似物是GH释放的有效刺激剂,在临床医学中有潜在应用。