1. GPCR/G Protein Neuronal Signaling
  2. Neuropeptide FF Receptor Opioid Receptor
  3. NPFF1-R antagonist 1

NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively.

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NPFF1-R antagonist 1 Chemical Structure

NPFF1-R antagonist 1 Chemical Structure

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Description

NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively[1].

IC50 & Target

NPFF1-R

211 ± 54 nM (Ki)

NPFF2-R

3270 ±639 nM (Ki)

κ Opioid Receptor/KOR

1390 ± 147 nM (Ki)

δ Opioid Receptor/DOR

1540 ± 132 nM (Ki)

μ Opioid Receptor/MOR

3560 ± 364 nM (Ki)

In Vitro

NPFF1-R antagonist 1 (compound 8b) shows some off target binding at the opioid receptors (DOR, KOR, and MOR), with Ki values of 1540 ± 132, 1390 ± 147, and 3560 ± 364 nM, respectively[1].
NPFF1-R antagonist 1 (0-10 μM) fails to inhibit cAMP stimulation, dose-dependently reverses NPFF inhibition of forskolin (HY-15371)-induced cAMP accumulation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

560.77

Formula

C37H44N4O

SMILES

O=C(CN1CCC(CC2=CC=CC=C2)CC1)NCC3(CCN(CC4=CC=CC=C4)CC3)NC5=C(C=CC=C6)C6=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
NPFF1-R antagonist 1
Cat. No.:
HY-161405
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