Pharmacological characterization of the mouse NPFF₂ receptor

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• 作者：Franck Talmont ; Lionel Moulé ; dous ; Laura Piedra-Garcia ; Martine Schmitt ; Fré ; dé ; ric Bihel ; Jean-Jacques Bourguignon ; Jean-Marie Zajac ; Catherine Mollereau
• 关键词：Neuropeptide FF ; Receptor ; Binding ; Species comparison
• 刊名：Peptides
• 出版年：2010
• 出版时间：February 2010
• 年：2010
• 卷：31
• 期：2
• 页码：215-220
• 全文大小：775 K

文摘

This study presents the binding and functional properties of the mouse NPFF₂ (mNPFF₂) receptor, in comparison with its human counterpart (hNPFF₂). Binding experiments were performed by using the NPFF₂ selective radioligand [³H]-EYF in membranes from CHO cells transfected with mouse and human NPFF₂ receptors and compared to membranes from mouse olfactory bulb, the brain region expressing the highest density of NPFF₂ receptors in mouse. mNPFF₂ receptors exhibited a high affinity (Kd = 0.2–0.4 nM) for [³H]-EYF, comparable to that of hNPFF₂ receptors. Also, the binding selectivity profile of mNPFF₂ receptors was comparable to that of hNPFF₂ 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 hNPFF₂ receptors, mNPFF₂ receptors were less discriminative towards the proNPFF_B-derived peptide. This suggests some species-related differences in the binding properties of NPFF₂ receptors that could have repercussion when evaluating the pharmacological properties of drugs in vivo.