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Search for the “ideal analgesic” in pain treatment by engineering the mu‐opioid receptor
Author(s) -
Tao PaoLuh,
Law PingYee,
Loh Horace H.
Publication year - 2010
Publication title -
iubmb life
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.132
H-Index - 113
eISSN - 1521-6551
pISSN - 1521-6543
DOI - 10.1002/iub.292
Subject(s) - analgesic , opioid , morphine , chronic pain , pharmacology , nociception , medicine , opioid receptor , addiction , receptor , drug , receptor antagonist , antagonist , bioinformatics , biology , psychiatry
The myriad of side effects that associate with morphine has been problematic in the clinical use to manage moderate to severe pain. It has been the holy grail of the pharmacologists to develop a compound, or treatment paradigm that could retain the analgesic effect of the drug as eliminating or reducing the side effects, mainly the tolerance and addiction development associates with chronic usage of the drug. In our earlier receptor structure/activities studies, we discovered an unique mutation of a conserved Ser in the fourth transmembrane domain of the opioid receptor that the alkaloid antagonist could activate the receptor. On the basis of this initial finding, we decide to explore the possibility of using virus to deliver the mutant mu‐opioid receptor at the various sites of the nociceptive pathway and induce the antinociceptive responses with the systemic administration of opioid antagonists. In this article, we will summarize the progress of such approach and the probable advantages over the conventional approach of drug development in the treatment of chronic pain. © 2009 IUBMB IUBMB Life, 62(2): 103–111, 2010