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Deltorphin transport across the blood-brain barrier.
| Content Provider | Semantic Scholar |
|---|---|
| Author | Fiori, Alessandro Cardelli, Patrizia Negri, Lucia Savi, Monia Strom, Roberto Erspamer, Vittorio |
| Copyright Year | 1997 |
| Abstract | In vivo antinociception studies demonstrate that deltorphins are opioid peptides with an unusually high blood-brain barrier penetration rate. In vitro, isolated bovine brain microvessels can take up deltorphins through a saturable nonconcentrative permeation system, which is apparently distinct from previously described systems involved in the transport of neutral amino acids or of enkephalins. Removing Na+ ions from the incubation medium decreases the carrier affinity for deltorphins (-25%), but does not affect the Vmax value of the transport. The nonselective opiate antagonist naloxone inhibits deltorphin uptake by brain microvessels, but neither the selective delta-opioid antagonist naltrindole nor a number of opioid peptides with different affinities for delta- or mu-opioid receptors compete with deltorphins for the transport. Binding studies demonstrate that mu-, delta-, and kappa-opioid receptors are undetectable in the microvessel preparation. Preloading of the microvessels with L-glutamine results in a transient stimulation of deltorphin uptake. Glutamine-accelerated deltorphin uptake correlates to the rate of glutamine efflux from the microvessels and is abolished by naloxone. |
| Starting Page | 1304 |
| Ending Page | 1308 |
| Page Count | 5 |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | http://www.pnas.org/content/94/17/9469.full.pdf |
| PubMed reference number | 9256506v1 |
| Volume Number | 94 |
| Issue Number | 17 |
| Journal | Proceedings of the National Academy of Sciences of the United States of America |
| Language | English |
| Access Restriction | Open |
| Subject Keyword | Amino Acids, Neutral Blood - brain barrier anatomy Bos taurus Enkephalins Glutamine Gonadotropin-Releasing Hormone Receptor Iontophoresis Microvessels Naloxone Narcotic Antagonists Opiates Opioid Peptide Opioid Receptor Opioids Receptors, Opioid, kappa Sodium deltorphin naltrindole |
| Content Type | Text |
| Resource Type | Article |
