Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 13, Issue 24, Pages 6713-6717Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2005.07.051
Keywords
antinociceptive activity; binding studies; mu-opioid receptor agonists
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In this paper, we describe the synthesis of a series of endomorphin-2 analogs containing N-methylated amino acids, consecutively in each position. The mu-opioid receptor binding affinities of the new analogs were determined in the displacement experiments. Their in vivo antinociceptive activity was assessed in the hot-plate test in mice after central (icv) and peripheral (ip) administration. [Sar(2)]endomorphin-2, which had the highest mu-receptor affinity, also showed the strongest analgesic effect when administered centrally and was the only analog that retained activity after peripheral injection. (c) 2005 Elsevier Ltd. All rights reserved.
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