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. 2015 Jun 24;3:40. doi: 10.3389/fchem.2015.00040

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Copyright © 2015 Jones and Polt.

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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I.v. activity of DAMGO analogs vs. ampipathicity from Lowery et al. (2007). A series of DAMGO analogs [in order of increasing hydrophilicity: DAMGO, DAMGO-Ser(OH), DAMGO-Ser(OXyl), DAMGO-Ser(OGlc), DAMGO-Ser(OLac)] were tested for i.v. MOR activity using mouse tail-flick tests (Lowery et al., 2007). It was observed that initial increases to hydrophilicity significantly improved activity, but subsequent increases led to a decrease. This is believed to be the result of the peptides spending a preponderance of time in the aqueous phase, providing reduced opportunities for MOR binding and activation.