Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain
| Autor: | Richard J. Knapp, Frank Porreca, Ewa Malatynska, Victor J. Hruby, Ferenc Ötvös, Mark S. Yamamura, Geza Toth, Henry I. Yamamura, Robert Horvath |
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| Rok vydání: | 1992 |
| Předmět: |
Male
Indoles Stereochemistry Binding Competitive General Biochemistry Genetics and Molecular Biology Naltrindole Receptors Opioid delta medicine Ic50 values Radioligand Animals General Pharmacology Toxicology and Pharmaceutics Receptor Membranes Chemistry Antagonist Brain Rats Inbred Strains General Medicine Rat brain Naltrexone Rats Dissociation constant Morphinans Opioid Receptors Opioid medicine.drug |
| Zdroj: | Life Sciences. 50:PL119-PL124 |
| ISSN: | 0024-3205 |
| DOI: | 10.1016/0024-3205(92)90464-z |
| Popis: | [3H]Naltrindole binding characteristics were determined using homogenized rat brain tissue. Saturation binding studies at 25 degrees C measured an equilibrium dissociation constant (Kd) value of 37.0 +/- 3.0 pM and a receptor density (Bmax) value of 63.4 +/- 2.0 fmol/mg protein. Association binding studies showed that equilibrium was reached within 90 min at a radioligand concentration of 30 pM. Naltrindole, as well as the ligands selective for delta (delta) opioid receptors, such as pCI-DPDPE and Deltorphin II inhibited [3H]naltrindole binding with nanomolar IC50 values. Ligands selective for mu (mu) and kappa (kappa) opioid receptors were only effective in inhibiting [3H]naltrindole binding at micromolar concentrations. From these data, we conclude that [3H]naltrindole is a high affinity, selective radioligand for delta opioid receptors. |
| Databáze: | OpenAIRE |
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