Description
An NPFF receptor antagonist; binds to human NPFF1 and NPFF2 receptors (Kis = 58 and 75 nM, respectively); selective for NPFF1 and NPFF2 receptors over NPY receptor Y1, GPR10, GPR54, GPR103, ORL-1, and μ-, δ-, and κ-opioid receptors at 10 μM; inhibits NPFF-induced [35S]GTPγS binding to the NPFF2 receptor at 7.5 μM; reverses NPVF-induced inhibition of forskolin-stimulated cAMP accumulation in CHO cells expressing the human NPFF1 receptor (EC50 = 4.7 μM); inhibits NPFF-induced increases in mean arterial pressure and heart rate in rats at 10 μg, i.c.v.; prevents heroin-induced delayed hyperalgesia and associated tolerance in rats at 0.1 mg/kg, s.c.
Formal name: N2-(tricyclo[3.3.1.13,7]dec-1-ylcarbonyl)-L-arginyl-L-phenylalaninamide
Synonyms:
Molecular weight: 482.6
CAS: 876310-60-0
Purity: ≥98%
Formulation: A solid
