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NPFF1-R antagonist 1 (compound 8b) is a piperidine analog and an effective neuropeptide FF (NPFF) receptor antagonist. It exhibits 15-fold selectivity for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively.

| Description | NPFF1-R antagonist 1 (compound 8b) is a piperidine analog and an effective neuropeptide FF (NPFF) receptor antagonist. It exhibits 15-fold selectivity for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively. |
| Targets&IC50 | κ opioid receptor:1390 ± 147 nM (Ki), NPFF1R:211 ± 54 nM (Ki), NPFF2R:3270 ±639 nM (Ki) |
| In vitro | NPFF1-R antagonist 1 (compound 8b) exhibits off-target binding at the opioid receptors (DOR, KOR, and MOR), with K i values of 1540 ± 132, 1390 ± 147, and 3560 ± 364 nM, respectively. At concentrations of 0-10 μM, NPFF1-R antagonist 1 does not inhibit cAMP stimulation but dose-dependently reverses the NPFF-induced inhibition of forskolin-induced cAMP accumulation. |
| Formula | C37H44N4O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |

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