TABLE 1

Brain and blood levels of 6-MAM (% of control) 5 and 25 min after a single heroin or 6-MAM injection (1.25–2.5 μmol/kg, s.c.) in mice pretreated with anti-6-MAM mAb (10–100 mg/kg, i.p.) 48 hours prior to opioid injection. Total drug doses are on the basis of administration to a 25-g mouse (n = 5–14).

Drug DoseTotal Drug DosemAb DoseTotal mAb Binding SitesDrug/mAb Binding SitesBrain 6-MAMBlood 6-MAM
5 min25 min5 min25 min
μmol/kgnmolmg/kgnmolratio% of control% of control% of control% of control
Heroin2.562.5103.31973 ± 1344 ± 3***117 ± 2294 ± 11
2.562.55016.74n.m.21 ± 2***n.m.62 ± 11
2.562.510033.32n.m.23 ± 3***n.m.74 ± 13
1.2531.310033.3163 ± 10n.m.330 ± 67**n.m.
6-MAM2.562.5103.31943 ± 12**32 ± 3***101 ± 1771 ± 11*
2.562.55016.74n.m.12 ± 1***n.m.42 ± 18**
2.562.510033.32n.m.10 ± 2***n.m.158 ± 34
1.2531.310033.3126 ± 7*n.m.307 ± 64*n.m.
  • n.m., not measured; Mann-Whitney U test; *P < 0.05, **P < 0.01, ***P < 0.001.