Abstract：
:Morphine and oxycodone are potent opioid analgesics most commonly used for the management of moderate to severe acute and chronic pain. Their clinical utility is limited by undesired side effects like analgesic tolerance, dependence, and withdrawal. We have previously demonstrated that endothelin-A (ETA) receptor antagonists potentiate opioid analgesia and eliminate analgesic tolerance. Mechanistically, G proteins and regulatory proteins such as β-arrestins have shown to play an important role in mediating opioid tolerance, dependence, and withdrawal. Recently, the involvement of central ET mechanisms in opioid withdrawal was investigated. ETA receptor antagonist was shown to block majority of the signs and symptoms associated with opioid withdrawal. This review focuses on ET as one of the potential novel strategies to manage the challenge of opioid withdrawal. An overview of additional players in this process (G proteins and β-arrestin2), and the possible therapeutic implications of these findings are presented.
journal_name
Life Scijournal_title
Life sciencesauthors
Bhalla S,Andurkar SV,Gulati Adoi
10.1016/j.lfs.2016.01.016subject
Has Abstractpub_date
2016-08-15 00:00:00pages
34-42eissn
0024-3205issn
1879-0631pii
S0024-3205(16)30016-9journal_volume
159pub_type
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