TABLE 3

Summary of the antagonistic potency of bupropion and bupropion hydroxy metabolites on different pharmacological actions of nicotine after subcutaneous administration in mice

Results are presented as AD50 values (┬▒CL) calculated from the dose response. Each dose group included 8 to 12 animals.

Pharmacological Effect Bupropion (2RS,3RS)-Hydroxybupropion (2S,3S)-Hydroxybupropion (2R,3R)-Hydroxybupropion
mg/kg
Tail-flick 2.0 (1.8-3.6) 1.5 (0.6-3.8) 0.2 (0.1-0.3)a 2.5 (0.8-3.5)
Hot-plate 7.0 (5.9-9.5) 5.5 (3.6-16) 1.0 (0.2-5.2) 10.3 (8.0-12)
Hypomotility 3.0 (2.5-6.3) 8.2 (4-17.3) 0.9 (0.3-3.0)a >20
Hypothermia 7.5 (3-15.4) 19.4 (10-35) 1.5 (0.8-3.0)a >20
  • <>a P < 0.05 relative to (2RS,3RS)-hydroxybupropion.