RFRP-1(human)

RFRP-1(human) is a gonadotropin-inhibitory hormone (GnIH) homolog. RFRP-1(human) targets human gonadotropin-releasing hormone (GnRH) neurons and gonadotropes and potently inhibits gonadotropin. RFRP-1(human) is a potent Neuropeptide FF (NPFF) receptor agonist with EC50s of 0.0011 nM and 29 nM for NPFF2 and NPFF1, respectively[1][2][3].

NC([C@H](CC1=CC=CC=C1)NC([C@H](CCCNC(N)=N)NC([C@H](CC(C)C)NC([C@H]2N(CCC2)C([C@H](CC(C)C)NC([C@H](CC(N)=O)NC([C@H](C)NC([C@@H](NC([C@H](CO)NC([C@H](CC3=CN=CN3)NC([C@H]4N(CCC4)C([C@@H](N)CCSC)=O)=O)=O)=O)CC5=CC=CC=C5)=O)=O)=O)=O)=O)=O)=O)=O

[1]Takayoshi Ubuka, et al. Identification of human GnIH homologs, RFRP-1 and RFRP-3, and the cognate receptor, GPR147 in the human hypothalamic pituitary axis. PLoS One. 2009 Dec 22;4(12):e8400.|[2]R Nichols, et al. Human RFamide-related peptide-1 diminishes cellular and integrated cardiac contractile performance. Peptides. 2010 Nov;31(11):2067-74.|[3]C Gouardères, et al. Functional differences between NPFF1 and NPFF2 receptor coupling: high intrinsic activities of RFamide-related peptides on stimulation of [35S]GTPgammaS binding. Neuropharmacology. 2007 Feb;52(2):376-86.