An NPFF receptor antagonist; binds to human NPFF1 and NPFF2 receptors (Kis = 58 and 75 nM

RF9 – 5 mg

Brand:
Cayman
CAS:
876310-60-0
Storage:
-20
UN-No:
Non-Hazardous - /

RF9 is a neuropeptide FF (NPFF) receptor antagonist.{57271} It binds to human NPFF1 and NPFF2 receptors with Ki values of 58 and 75 nM, respectively. It is selective for NPFF1 and NPFF2 receptors over neuropeptide Y (NPY) receptor Y1, GPR10, GPR54, GPR103, ORL-1, and μ-, δ-, and κ-opioid receptors at 10 μM. RF9 (7.5 μM) inhibits NPFF-induced [35S]GTPγS binding to the NPFF2 receptor. It reverses NPVF-induced inhibition of forskolin-stimulated cAMP accumulation in CHO cells expressing the human NPFF1 receptor (EC50 = 4.7 μM). Intracerebroventricular administration of RF9 (10 μg) inhibits NPFF-induced increases in mean arterial pressure and heart rate in rats. It prevents heroin-induced delayed hyperalgesia and associated tolerance in rats when administered subcutaneously at a dose of 0.1 mg/kg.  

 

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SKU: 31412 - 5 mg Category:

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

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