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. Author manuscript; available in PMC: 2022 Oct 24.
Published in final edited form as: J Med Chem. 2020 Jul 31;63(21):12387–12402. doi: 10.1021/acs.jmedchem.0c00643

Table 3.

Binding affinity and relative potency to reverse morphine-induced analgesia of representative NPFF peptidic analogues.77

Compound Binding affinity Ki (nM)a Minimal effective dose (nmol)b
NPFF 0.21 ± 0.03 22
[Tyr1]NPFF 0.20 ± 0.04 8.8
[Gly5]NPFF 1.2 ± 0.2 8.8
a

Affinity for rat spinal cord membranes using [125I][Tyr1]NPFF tracer.

b

Mimimal effective dose (i.c.v.) able to significantly reverse morphine-induced analgesia.