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RFRP-3 (Neuropeptide VF(124-131))(human), a human GnIH peptide homolog, is a potent inhibitor of gonadotropin secretion by inhibiting Ca mobilization. RFRP-3(human) is a NPFF1 receptor agonist, it inhibits forskolin-induced production of cAMP with an IC₅₀ of 0.7 nM.

RFRP-3 efficiently inhibits forskolin-induced production of cAMP with an IC₅₀ of 0.7 nM.
Scatchard-plot analysis shows that I-labelled hRFRP-3 has a single class of high-affinity binding sites for the membrane fractions of CHO cells expressing rat OT7T022, the K_d value and the B_max values are 0.19 nM and 1.3 pM, respectively.
RFRP-3 specifically stimulate cells transfected with a new orphan 7TMR, OT7T022, it binds to OT7T022 as a specific ligand with high affinity (K_d= 0.19 nM).
RFRP-3 (10 to 10M) has no effect on LH and FSH levels alone, but when it combines with GnRH, LH and FSH secretion is significantly reduced by the combination.

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