Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Doi, N. et al.

Doi, Hirotani, Ukai, Shimada, Okuno, Kurasaki, Kiyofuji, Ikegami, Futamata, Nakagawa, Ase, Chihara,

Pharmacological characteristics of KP-102 (GHRP-2), a potent growth hormone-releasing peptide.

KP-102 (D-alanyl-3-(2-naphthyl)-D-alanyl-L-alanyl-L-tryptophyl-D-phenylalanyl-L-lysinamide dihydrochloride, growth hormone-releasing peptide-2, GHRP-2, pralmorelin, CAS 158861-67-7), is a potent synthetic growth hormone ( GH) secretagogue. In the present study, the pharmacological characteristics of the GH-releasing property of KP-102 were investigated by means of in vivo and in vitro experiments. In conscious rats, the GH-releasing activity of KP-102 was more potent than that of exogenously injected GH-releasing hormone (GHRH). Under pentobarbital anesthesia in which endogenous somatostatin secretion is known to be decreased, KP-102 and GHRH, both showed an almost equivalent GH-releasing potency, which was also similar to that of KP-102 in conscious rats. Besides, KP-102 showed GH-releasing activity in conscious dogs as well, while GHRH failed to increase serum GH levels in conscious dogs. These findings suggest that the GH- releasing activity of KP-102 was less sensitive to GH suppression by endogenous somatostatin as compared with that of GHRH. The GH-releasing activity of KP-102 was completely absent in hypophysectomized rats, but present in median eminence-lesioned rats in which secreted GH amounts were significantly less than those normal rats, indicating necessity of the median eminence (endogenous GHRH) to exert the full activity of KP-102 in GH stimulation. KP-102 directly stimulated GH secretion from cultured rat anterior pituitary cells, although the GH- releasing potency of KP-102 was significantly weaker than that of GHRH in vitro. In conscious rats, KP-102 stimulated the secretion of both adrenocorticotrophic hormone (ACTH) and corticosterone, but not of prolactin. Three weeks administration of KP-102 showed growth-accelerating effect, a slight increase of body weight and wet weight of some organs in both normal and monosodium glutamate (MSG)-treated rats. These results suggest that KP-102 showed specific GH-releasing activity apart from slight ACTH secretion, and that the GH- releasing activity was stable in comparison with that of exogenously injected GHRH.[1]

References

Pharmacological characteristics of KP-102 (GHRP-2), a potent growth hormone-releasing peptide. Doi, N., Hirotani, C., Ukai, K., Shimada, O., Okuno, T., Kurasaki, S., Kiyofuji, T., Ikegami, R., Futamata, M., Nakagawa, T., Ase, K., Chihara, K. Arzneimittel-Forschung. (2004) [Pubmed]

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