Bowers C Y
Tulane University Medical Center, New Orleans, LA 70112.
J Pediatr Endocrinol. 1993 Jan-Mar;6(1):21-31. doi: 10.1515/jpem.1993.6.1.21.
A new class of small synthetic peptides has been developed which specifically release GH. They consist of 6-7 amino acids and release GH in animals as well as humans. So far 3 of these peptides have been administered to humans, i.e., GHRP-6, GHRP-1 and GHRP-2. As in rats, these 3 peptides have been found to be increasingly more effective in releasing GH in humans. All 3 GHRPs release GH more efficaciously than GHRH 1-44 NH2 in humans. Particularly note-worthy is that GHRP-6, GHRP-1 AND GHRP-2 all release GH after oral administration. Near maximal amounts of GH can be released after GHRP-1 and GHRP-2 oral administration. In the present studies, the GH responses and serum irGHRP levels after i.v., s.c. and oral administration have been determined in normal younger men and/or women. By each route of administration GH was very effectively released. Additionally, GH release was induced by oral GHRP-6 in children with various degrees of GH deficiency. Noteworthy is the synergistic release of GH induced by the combined i.v. bolus administration of 1 microgram/kg of GHRP-1 + GHRH 1-44NH2. Thus, these results demonstrate GHRPs' potential importance at the theoretical as well as pharmaceutical level.
已开发出一类新型的小分子合成肽，它们能特异性释放生长激素（GH）。这些肽由6 - 7个氨基酸组成，在动物和人类中均可释放GH。到目前为止，其中3种肽已应用于人体，即生长激素释放肽-6（GHRP - 6）、生长激素释放肽-1（GHRP - 1）和生长激素释放肽-2（GHRP - 2）。与在大鼠中一样，已发现这3种肽在人体中释放GH的效果越来越好。在人体中，所有这3种生长激素释放肽（GHRP）释放GH的效果都比生长激素释放激素（GHRH）1 - 44 NH2更有效。特别值得注意的是，GHRP - 6、GHRP - 1和GHRP - 2口服后均可释放GH。口服GHRP - 1和GHRP - 2后可释放接近最大量的GH。在本研究中，已测定了正常年轻男性和/或女性静脉注射、皮下注射和口服后生长激素（GH）的反应以及血清免疫反应性生长激素释放肽（irGHRP）水平。通过每种给药途径，GH都能非常有效地释放。此外，口服GHRP - 6可诱导不同程度生长激素缺乏儿童释放GH。值得注意的是，静脉推注1微克/千克的GHRP - 1与GHRH 1 - 44NH2联合给药可诱导GH的协同释放。因此，这些结果证明了生长激素释放肽在理论和制药层面的潜在重要性。
