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Development of sub-nanomolar dipeptidic ligands of neuropeptide FF receptors.

Abstract：

:Based on our earlier reported neuropeptide FF receptors antagonist (RF9), we carried out an extensive structural exploration of the N-terminus part of the amidated dipeptide Arg-Phe-NH(2) in order to establish a structure-activity relationships (SAR) study towards both NPFF receptor subtypes. This SAR led to the discovery of dipeptides (12, 35) with subnanomolar affinities towards NPFF1 receptor subtype, similar to endogenous ligand NPVF. More particularly, compound 12 exhibited a potent in vivo preventive effect on opioid-induced hyperalgesia at low dose. The significant selectivity of 12 toward NPFF1-R indicates that this receptor subtype may play a critical role in the anti-opioid activity of NPFF-like peptides.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Gealageas R,Schneider S,Humbert JP,Bertin I,Schmitt M,Laboureyras E,Dugave C,Mollereau C,Simonnet G,Bourguignon JJ,Simonin F,Bihel F

doi

10.1016/j.bmcl.2012.10.049

subject

Has Abstract

pub_date

2012-12-15 00:00:00

pages

7471-4

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01327-3

journal_volume

22

pub_type

杂志文章

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