Abstract：
:This study presents the binding and functional properties of the mouse NPFF(2) (mNPFF(2)) receptor, in comparison with its human counterpart (hNPFF(2)). Binding experiments were performed by using the NPFF(2) selective radioligand [(3)H]-EYF in membranes from CHO cells transfected with mouse and human NPFF(2) receptors and compared to membranes from mouse olfactory bulb, the brain region expressing the highest density of NPFF(2) receptors in mouse. mNPFF(2) receptors exhibited a high affinity (Kd=0.2-0.4 nM) for [(3)H]-EYF, comparable to that of hNPFF(2) receptors. Also, the binding selectivity profile of mNPFF(2) receptors was comparable to that of hNPFF(2) receptors, except for three ligands (NPSF, NPVF, RF9) that were about tenfold more potent and active on mouse receptors than on human receptors. In particular, compared to hNPFF(2) receptors, mNPFF(2) receptors were less discriminative towards the proNPFF(B)-derived peptide. This suggests some species-related differences in the binding properties of NPFF(2) receptors that could have repercussion when evaluating the pharmacological properties of drugs in vivo.
journal_name
Peptidesjournal_title
Peptidesauthors
Talmont F,Moulédous L,Piedra-Garcia L,Schmitt M,Bihel F,Bourguignon JJ,Zajac JM,Mollereau Cdoi
10.1016/j.peptides.2009.11.020subject
Has Abstractpub_date
2010-02-01 00:00:00pages
215-20issue
2eissn
0196-9781issn
1873-5169pii
S0196-9781(09)00511-7journal_volume
31pub_type
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