Effects of β-funaltrexamine on radiolabeled opioid binding Journal Article
| Authors: | Recht, L. D.; Pasternak, G. W. |
| Article Title: | Effects of β-funaltrexamine on radiolabeled opioid binding |
| Abstract: | β-Funaltrexamine (β-FNA) potently competed with the binding of a series of radiolabeled opiates and opioid peptides in standard binding assays with IC50 values under 10 nM. In addition, higher concentrations of β-FNA produced an irreversible inhibition of binding which was relatively selective for μ receptors: δ binding was not affected much. The production of irreversible inhibition of [3H]dihydromorphine binding required concentrations of β-FNA over 10-fold higher than β-FNA concentrations needed in standard competition studies. Both μ1 and μ2 sites were irreversibly inhibited by β-FNA, but μ1 sites were more sensitive. The reversible and irreversible inhibition in these in vitro binding assays by β-FNA were quite similar to naloxonazine. However, the activity of β-FNA in the guinea-pig ileum suggests that it may not distinguish between μ1 and gm2 receptors as effectively as naloxonazine in bioassays and in vivo. © 1987. |
| Keywords: | nonhuman; animal cell; animal; central nervous system; drug receptor binding; drug antagonism; brain; rat; rats; radioisotope; morphine; receptors, opioid, mu; drug binding; pharmacokinetics; in vitro; naloxone; opiate receptor; beta funaltrexamine; naltrexone; binding, competitive; naloxonazine; opiate derivative; opiate receptors; rats, inbred strains; narcotic antagonists; receptors, opioid; β-funaltrexamine; male; priority journal; dihydromorphine; enkephalin, leucine-2-alanine; support, u.s. gov't, p.h.s.; enkephalin, leucine; μ1-receptors |
| Journal Title: | European Journal of Pharmacology |
| Volume: | 140 |
| Issue: | 2 |
| ISSN: | 0014-2999 |
| Publisher: | Elsevier B.V. |
| Date Published: | 1987-08-11 |
| Start Page: | 209 |
| End Page: | 214 |
| Language: | English |
| DOI: | 10.1016/0014-2999(87)90807-7 |
| PUBMED: | 2822439 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Article -- Export Date: 5 February 2021 -- Source: Scopus |
