Galanin and its three receptors have been linked to a wide variety of physiological processes and are distributed in both the central and peripheral nervous systems. Further knowledge of the properties of galanin-activated signaling systems can best be obtained by the availability of peptide and non-peptide ligands that are selective for the different receptor subtypes. The current study describes binding and signaling data for the chimeric peptide, galanin-(2–13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide (M871). This compound binds to the galanin receptor type 2 with more than 30-fold higher affinity than to the galanin receptor type 1 and exhibits antagonist actions at galanin receptor type 2, blocking increased release of inositol phosphate produced by galanin in CHO cells. This peptide opens new possibilities for the study of galanin receptor physiology.
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This work was supported by grants from the Swedish Research Council (VR-Med).
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Sollenberg, U., Lundström, L., Bartfai, T. et al. M871—A Novel Peptide Antagonist Selectively Recognizing the Galanin Receptor Type 2 . Int J Pept Res Ther 12, 115–119 (2006). https://doi.org/10.1007/s10989-005-9008-x
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DOI: https://doi.org/10.1007/s10989-005-9008-x