| Description | RF9 acetate is an effective and selective antagonist of Neuropeptide FF receptor with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively. |
| In vitro | 在Neuro 2A细胞中，预处理RF9 acetate（10 μM）能完全阻断NPFF诱导的神经突生长[2]。 |
| In vivo | RF9 acetate (10 μg)单独注入不会显著改变MAP或心率。相反，当 RF9 acetate 与NPFF一起应用时，由NPFF引起的MAP和心率增加被显著阻断。 RF9 acetate (0.1 mg/kg, s.c.，在0.3 mg/kg海洛因或生理盐水前)与海洛因共同使用，可预防海洛因引起的延迟性高痛敏和耐受性[2]。 |
| Target activity | NPFF1 (human):58 nM (Ki), NPFF2 (human):75 nM (Ki) |
| molecular weight | 542.67 |
| Molecular formula | C28H42N6O5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (101.35 mM) |
| References | 1. Ting Zhang, et al. Discovery of Two Novel Branched Peptidomimetics Containing endomorphin-2 and RF9 Pharmacophores: Synthesis and Neuropharmacological Evaluation. Bioorg Med Chem. 2019 Feb 15;27(4):630-643. 2. Simonin F, et al. RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia. Proc Natl Acad Sci U S A. 2006 Jan 10;103(2):466-71. |