Supraspinal μ(2)-opioid receptors mediate spinal/supraspinal morphine synergy Journal Article
| Authors: | Pick, C. G.; Roques, B.; Gacel, G.; Pasternak, G. W. |
| Article Title: | Supraspinal μ(2)-opioid receptors mediate spinal/supraspinal morphine synergy |
| Abstract: | TRIMU-5 (Tyr-D-Ala-Gly-NHC2H4CH(CH3)2) is a potent μ2-opioid agonist/μ1-opioid antagonist. A supraspinal dose (0.5 μg i.c.v.) of TRIMU-5 which is not analgesic when given alone antagonizes the analgesia produced by intracerebroventricular (i.c.v.) morphine, a μ1 action. In contrast, in a synergy model consisting of the simultaneous administration of intrathecal morphine (0.1 μg) with multiple doses of i.c.v. morphine, the same supraspinal TRIMU-5 dose (0.5 μg i.c.v.) enhances analgesia. Supraspinal TRIMU-5 also potentiates spinal morphine directly, shifting its dose-response to the left. These results imply that within the brainstem μ1 receptors mediate supraspinal analgesia while μ2 receptors mediate the synergy with spinal μ systems. © 1992. |
| Keywords: | controlled study; unclassified drug; drug potentiation; nonhuman; mouse; animal; mice; animal experiment; dose-response relationship, drug; central nervous system; drug synergism; drug antagonism; spinal cord; morphine; oligopeptides; analgesia; brain stem; mu opiate receptor; receptors, opioid, mu; injections, spinal; receptor subtype; injections, intraventricular; opiate antagonist; opiate agonist; male; priority journal; article; support, u.s. gov't, p.h.s.; μ-opioid receptors; trimu 5 |
| Journal Title: | European Journal of Pharmacology |
| Volume: | 220 |
| Issue: | 2-3 |
| ISSN: | 0014-2999 |
| Publisher: | Elsevier B.V. |
| Date Published: | 1992-09-22 |
| Start Page: | 275 |
| End Page: | 277 |
| Language: | English |
| DOI: | 10.1016/0014-2999(92)90761-r |
| PUBMED: | 1330618 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Article -- Export Date: 30 July 2019 -- Source: Scopus |
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