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  • Title: Characterization of [3H]naltrindole binding to delta opioid receptors in rat brain.
    Author: Yamamura MS, Horvath R, Toth G, Otvos F, Malatynska E, Knapp RJ, Porreca F, Hruby VJ, Yamamura HI.
    Journal: Life Sci; 1992; 50(16):PL119-24. PubMed ID: 1313133.
    Abstract:
    [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.
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