Polyglycerol-opioid conjugate produces analgesia devoid of side effects.
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ABSTRACT:
SUBMITTER: Gonzalez-Rodriguez S
PROVIDER: S-EPMC5496737 | biostudies-literature | 2017 Jul
REPOSITORIES: biostudies-literature
Publications
Polyglycerol-opioid conjugate produces analgesia devoid of side effects.
González-Rodríguez Sara S Quadir Mohiuddin A MA Gupta Shilpi S Walker Karolina A KA Zhang Xuejiao X Spahn Viola V Labuz Dominika D Rodriguez-Gaztelumendi Antonio A Schmelz Martin M Joseph Jan J Parr Maria K MK Machelska Halina H Haag Rainer R Stein Christoph C
eLife 20170704
Novel painkillers are urgently needed. The activation of opioid receptors in peripheral inflamed tissue can reduce pain without central adverse effects such as sedation, apnoea, or addiction. Here, we use an unprecedented strategy and report the synthesis and analgesic efficacy of the standard opioid morphine covalently attached to hyperbranched polyglycerol (PG-M) by a cleavable linker. With its high-molecular weight and hydrophilicity, this conjugate is designed to selectively release morphine ...[more]
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