| Bioactivity | RF9 hydrochloride is a potent and selective Neuropeptide FF receptor antagonist, with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively[1][2]. |
| Invitro | RF9 (10 μM) pretrement completely blocks NPFF induced neurite outgrowth of Neuro 2A cells[2]. |
| In Vivo | RF9 (0.1 mg/kg, s.c. ) with heroin coadministration prevents heroin-induced delayed hyperalgesia and tolerance[1].RF9 (10 μg) infused alone does not result in a significant alteration of MAP or heart rate. Conversely, MAP and heart rate increases evoked by NPFF are significantly blocked when NPFF is applied in conjunction with RF9[1]. Animal Model: |
| Name | RF9 hydrochloride |
| Formula | C26H39ClN6O3 |
| Molar Mass | 519.08 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. 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. [2]. 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. |