RF 9 TFA

RF9 is a potent and selective Neuropeptide FF receptor antagonist, with Kis of 58±5 and 75±9 nM for hNPFF1R and hNPFF2R, respectively.

Signaling Pathways >> GPCR/G Protein >> Neuropeptide Y Receptor

Research Areas >> Cardiovascular Disease

Research Areas >> Neurological Disease

Ki: 58±5 nM (hNPFF1R), 75±9 nM (hNPFF2R)[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]. It is worthy to note that RF9 (30 nmol) significantly reduces the hypothermia induced by morphine (5 nmol)[2].

Rats: Rats (n=5) are catheterized for measurement of arterial blood pressure and receive an in-dwelling cannula into the lateral cerebral ventricle. Arterial blood pressure and heart rate are continuously monitored. NPFF (10 μg in 10 μL of saline) is injected into the lateral ventricle over 15 to 20 sec. Control injections of saline (10 μL) are carried out in the same animals. Upon return of blood pressure to baseline, RF9 (10 μg) is injected i.c.v., followed by another i.c.v. injection of NPFF with RF9. After 1.5 h., another i.c.v. infusion of NPFF is repeated[1].

[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]. Wang YQ, et al. Neuropeptide FF receptors antagonist, RF9, attenuates opioid-evoked hypothermia in mice. Peptides. 2008 Jul;29(7):1183-90.

Velneperit | MK 0557 | HT-2157 | BIIE 0246 | Galanin (1-16) (mouse, porcine, rat) | JNJ-31020028 | CGP 71683 HCl | FR252384 | Galanin (human) acetate salt | Galanin (1-13)-Substance P (5-11) amide | Galanin (1-13)-Pro-Pro-(Ala-Leu-)₂Ala amide | Neuropeptide Y (13-36) (human, rat) trifluoroacetate salt | Neuropeptide Y(29-64) | Pancreatic Polypeptide, bovine