Kappa(3) receptors and levorphanol-induced analgesia Journal Article
| Authors: | Tive, L.; Ginsberg, K.; Pick, C. G.; Pasternak, G. W. |
| Article Title: | Kappa(3) receptors and levorphanol-induced analgesia |
| Abstract: | Levorphanol is a widely used opiate analgesic. Although structurally related to morphine, levorphanol has high affinity for a number of receptor subtypes, including both kappa1, and kappa3. Prior reports had implicated a kappa component of levorphanol-induced antinociception. Evidence is now presented suggesting that levorphanol-induced analgesia is produced by a mixture of mu and kappa3 mechanisms. Levorphanol was a potent analgesic in the tail-flick assay, when given systemically, spinally or supraspinally. Isobolographic analysis of the combined administration of levorphanol, spinally and supraspinally implied synergistic interactions. Naloxonazine reduced levorphanol-induced analgesia, implicating a role for mu1 receptors. The kappa1 antagonist nor-binaltorphimine at a dose which reversed analgesia induced by U50,488H did not antagonize levorphanol-induced analgesia. Additional studies revealed no cross tolerance in either direction, between levorphanol with the kappa1 analgesic U50,488H. Together, these results strongly argue against a role for kappa1, receptors in levorphanol-induced analgesia. However, mice tolerant to the kappa3 analgesic, naloxone benzoylhydrazone (NalBzoH), showed cross tolerance to levorphanol, implying a role of kappa3 mechanisms in levorphanol-induced analgesia. © 1992. |
| Keywords: | controlled study; nonhuman; mouse; animal; mice; pain; animal experiment; dose-response relationship, drug; morphine; analgesics; analgesia; drug tolerance; levorphanol; reaction time; injections, intraventricular; 3,4 dichloro n methyl n [2 (1 pyrrolidinyl)cyclohexyl]benzeneacetamide methanesulfonate; naloxone benzoylhydrazone; kappa opiate receptor; naloxonazine; subcutaneous drug administration; intracerebroventricular drug administration; norbinaltorphimine; male; priority journal; article; receptors, opioid, kappa; support, u.s. gov't, p.h.s.; intrathecal drug administration; kappa receptors |
| Journal Title: | Neuropharmacology |
| Volume: | 31 |
| Issue: | 9 |
| ISSN: | 0028-3908 |
| Publisher: | Pergamon-Elsevier Science Ltd |
| Date Published: | 1992-09-01 |
| Start Page: | 851 |
| End Page: | 856 |
| Language: | English |
| DOI: | 10.1016/0028-3908(92)90121-5 |
| PUBMED: | 1331842 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Source: Scopus |
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