Comparison of naloxonazine and β-funaltrexamine antagonism of μ(1) and μ(2) opioid actions Journal Article
| Authors: | Pick, C. G.; Paul, D.; Pasternak, G. W. |
| Article Title: | Comparison of naloxonazine and β-funaltrexamine antagonism of μ(1) and μ(2) opioid actions |
| Abstract: | β-Funaltrexamine (β-FNA) irreversibly blocks morphine analgesia, lethality and its inhibition of gastrointestinal transit, confirming that these actions involve μ receptors. In dose-response studies, β-FNA antagonized all the actions with similar potencies (ID50 values of 12.1, 11.3 and 12.3 mg/kg, respectively). β-FNA also reduced intra-cerebroventricular and intrathecal DAMGO analgesia equally well (ID50 values of 6.09 and 7.7 mg/kg, respectively). Naloxonazine blocked systemic morphine analgesia (ID50 value 9.5 mg/kg) and supraspinal DAMGO analgesia (ID50 value 6.1 mg/kg) as potently as β-FNA. However, against spinal DAMGO analgesia, morphine's inhibition of gastro-intestinal transit or lethality, naloxonazine (ID50 values 38.8, 40.7 and 40.9 mg/kg, respectively) was significantly less active than β-FNA (p < 0.05). β-FNA remains a valuable tool in the classification of μ opioid actions. Within the μ category, actions can be defined as either μ1 (naloxonazine-sensitive) or μ2 (naloxonazine-insensitive). © 1991. |
| Keywords: | controlled study; nonhuman; comparative study; mouse; animal; mice; drug administration schedule; animal experiment; animalia; morphine; injections, subcutaneous; analgesia; receptors, opioid, mu; naloxone; opiate receptor; beta funaltrexamine; naltrexone; enkephalin, ala(2)-mephe(4)-gly(5)-; naloxonazine; enkephalin[2 dextro alanine 4 methylphenylalanine 5 glycine]; narcotic antagonists; subcutaneous drug administration; receptors, opioid; intracerebroventricular drug administration; male; priority journal; article; support, non-u.s. gov't; support, u.s. gov't, p.h.s.; enkephalins; intrathecal drug administration |
| Journal Title: | Life Sciences |
| Volume: | 48 |
| Issue: | 21 |
| ISSN: | 0024-3205 |
| Publisher: | Elsevier Inc. |
| Date Published: | 1991-01-01 |
| Start Page: | 2005 |
| End Page: | 2011 |
| Language: | English |
| DOI: | 10.1016/0024-3205(91)90155-5 |
| PUBMED: | 1851915 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Source: Scopus |
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