Functional antagonism of morphine analgesia by (+)-pentazocine: Evidence for an anti-opioid σ(1) system Journal Article
| Authors: | Chien, C. C.; Pasternak, G. W. |
| Article Title: | Functional antagonism of morphine analgesia by (+)-pentazocine: Evidence for an anti-opioid σ(1) system |
| Abstract: | Both (+)-pentazocine and (-)-pentazocine antagonize morphine analgesia equally well. This lack of stereospecificity implies an non-opioid mechanism of action. The antagonism of morphine analgesia by (+)-pentazocine is reversed by haloperidol, a potent dopamine D2 and σ receptor antagonist. The inactivity of the highly selective dopamine D2 receptor antagonist (-)-sulpiride indicates that both (+)-pentazocine and haloperidol are acting through σ receptors. Haloperidol, but not (-)-sulpiride, also enhances morphine analgesia. Together, these results suggest the presence of a tonically active anti-opioid σ system within the brain. © 1993. |
| Keywords: | controlled study; drug potentiation; nonhuman; mouse; animal; mice; haloperidol; animal experiment; drug antagonism; morphine; analgesia; drug interactions; stereoisomerism; receptor subtype; pentazocine; receptors, sigma; dopamine 2 receptor; subcutaneous drug administration; receptors, dopamine d2; male; priority journal; article; support, u.s. gov't, p.h.s.; sigma opiate receptor; sulpiride |
| Journal Title: | European Journal of Pharmacology |
| Volume: | 250 |
| Issue: | 1 |
| ISSN: | 0014-2999 |
| Publisher: | Elsevier B.V. |
| Date Published: | 1993-11-30 |
| Start Page: | R7 |
| End Page: | R8 |
| Language: | English |
| DOI: | 10.1016/0014-2999(93)90650-7 |
| PUBMED: | 8119306 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Source: Scopus |
