biological activity | RF9 is an effective and selective neuropeptide FF receptor (Neuropeptide FF receptor) antagonist, The Ki values for hNPFF1R and hNPFF2R are 58 and 7 nM respectively. |
target | hNPFF1R 58 nM (Ki) hNPFF2R 75 nM (Ki) |
in vitro study | RF9 (10 μM) pretrement completely blocks NPFF induced neurite outgrowth of Neuro 2A cells. |
in vivo study | RF9 (0.1 mg/kg, S. c. ) with hero coadministration prevents hero-induced delayed hyperalgesia and tolerance. 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. Animal Model: Rats. Dosage: 0.1 mg/kg. Administration: s.C. 30 min before 0.3 mg/kg nociceptive threshold in rat. Result: Opposed to delaye hero-induced hyperalgesia and associated tolerance. |
Animal Model:
| Rats. |
Dosage:
| 0.1 mg/kg. |
Administration:
| S.C. 30 min before 0.3 mg/kg heroin or saline on basal nociceptive threshold in rats. |
Result:
| Opposed to delaye heroin-induced hyperalgesia and associated tolerance. |