Morphine-6-glucuronide, a potent mu agonist Journal Article
| Authors: | Pasternak, G. W.; Bodnar, R. J.; Clark, J. A.; Inturrisi, C. E. |
| Article Title: | Morphine-6-glucuronide, a potent mu agonist |
| Abstract: | The 3- and the 6-glucuronides of morphine have been examined in binding studies and in vivo. The 3-glucuronide had poor affinity in all binding studies whereas the 6-glucuronide potently labeled mu, but not delta or kappa receptors with affinities similar to morphine. Microinjections of the 3-glucuronide directly into the periaqueductal gray were without effect. The 6-glucuronide, on the other hand, was up to 20-fold more potent than morphine following microinjections in the same region. High doses of the 6-glucuronide produced profound seizure activity. All 6-glucuronide actions were sensitive to the opiate antagonist naloxone. © 1987. |
| Keywords: | unclassified drug; nonhuman; animal; animal experiment; drug receptor binding; rat; rats; drug metabolism; radioisotope; morphine; analgesia; receptors, opioid, mu; pharmacokinetics; naloxone; microinjections; opiate receptor; morphine 6 glucuronide; biotransformation; receptors, opioid, delta; rats, inbred strains; morphine derivatives; receptors, opioid; male; support, non-u.s. gov't; support, u.s. gov't, p.h.s.; preliminary communication; enkephalin derivative h 3; ethylketazocine h 3; morphine 3 glucuronide |
| Journal Title: | Life Sciences |
| Volume: | 41 |
| Issue: | 26 |
| ISSN: | 0024-3205 |
| Publisher: | Elsevier Inc. |
| Date Published: | 1987-12-28 |
| Start Page: | 2845 |
| End Page: | 2849 |
| Language: | English |
| DOI: | 10.1016/0024-3205(87)90431-0 |
| PUBMED: | 2826951 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Article -- Export Date: 5 February 2021 -- Source: Scopus |
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