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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | D'amato, R. Holaday, J. W. |
| Abstract | The use of selective delta and mu opioid antagonists has provided evidence that delta opioid receptors within the brain mediate the endogenous opioid component of endotoxic shock hypotension. The selectivity of these delta and mu antagonists was demonstrated by their differing effects upon morphine analgesia and endotoxic hypotension. The mu antagonist beta-funaltrexamine, at doses that antagonized morphine analgesia, failed to alter shock, whereas the delta antagonist M 154,129: [N,N-bisallyl-Tyr-Gly-Gly-psi-(CH2S)-Phe-Leu-OH] (ICI) reversed shock at doses that failed to block morphine analgesia. Therefore, selective delta antagonists may have therapeutic value in reversing circulatory shock without altering the analgesic actions of endogenous or exogenous opioids. Additional data revealed that prior occupancy of mu binding sites by irreversible opioid antagonists may allosterically attenuate the actions of antagonists with selectivity for delta binding sites. For endogenous opioid systems, this observation provides an opportunity to link in vivo physiological responses with receptor-level biochemical interactions. |
| ISSN | 00278424 |
| e-ISSN | 10916490 |
| Journal | Proceedings of the National Academy of Sciences of the United States of America |
| Issue Number | 9 |
| Volume Number | 81 |
| Language | English |
| Publisher | National Academy of Sciences |
| Publisher Date | 1984-06-01 |
| Publisher Place | United States |
| Access Restriction | Open |
| Subject Keyword | Receptors, Opioid Physiology Shock, Septic Physiopathology Allosteric Regulation Animals Blood Pressure Drug Effects Enkephalin, Leucine Analogs & Derivatives Pharmacology Macromolecular Substances Naltrexone Receptors, Opioid, Delta Receptors, Opioid, Mu Multidisciplinary |
| Content Type | Text |
| Resource Type | Article |
| Subject | Multidisciplinary |
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