TABLE 1

Relative affinity of SNC-80 and enkephalins for hDOR in SK-N-BE cells

Ki1 and Ki2 values, corresponding to high- and low-affinity sites, respectively, were determined from competition of [3H]diprenorphine binding by SNC-80, Leu-, and Met-enkephalin. Data are means ± S.E.M. from three different experiments performed in triplicate.


Agonist

Binding Ki

Percentage of Each Site
nM
SNC-80 Ki1 = 0.10 ± 0.01 54.5 ± 5.7
Ki2 = 54.1 ± 19.5 45.5 ± 4.3
Leu-enkephalin Ki1 = 0.18 ± 0.03 63.4 ± 5.1
Ki2 = 54.4 ± 9.0 36.6 ± 4.9
Met-enkephalin Ki1 = 1.01 ± 0.18* 74.9 ± 5.2

Ki2 = 115 ± 34
25.1 ± 4.8
  • * Significantly different from SNC-80 and Leu-enkephalin; p < 0.01, ANOVA followed by Bonferroni-Dunn test.