Table 5

Maximum stimulation and inhibition of spontaneous locomotor activity by pyrazole analogs

CompoundCompound AloneCompound with 3 mg/kg Δ9-THC
Max Stim (Dose)Max % Inhibit (Dose)Max Stim (Dose)Max % Inhibit (Dose)
3-Substituent
 O-848None (10)69% (10)N.T.N.T.
 O-84925% (10)48% (30)N.T.N.T.
 O-850None (10)43% (10)N.T.N.T.
 O-85252% (1)Stim at 1, 3, and 10N.T.N.T.
 O-853N.T.N.T.N.T.N.T.
 O-869None (30)31% (30)N.T.N.T.
 O-870None (30)46% (30)N.T.N.T.
 O-88931% (1)96% (30)None (3)72% (3)
 O-8904% (30)Stim at 30N.T.N.T.
 O-909None (30)3% (30)N.T.N.T.
 O-9104% (30)Stim at 30N.T.N.T.
 O-104324% (3)49% (30)None (3 and 10)88% (3)
 O-12697% (1)87% (30)None (1, 3, and 10)91% (10)
 O-127029% (3)80% (30)None (10)87% (10)
 O-127154% (3)7% (30)None (3 and 10)58% (3)
 O-127217% (3)54% (30)N.T.N.T.
 O-1398None (3, 10, and 30)97% (10)N.T.N.T.
 O-1399None (3, 10, and 30)100% (30)N.T.N.T.
 O-1876None (30)11% (30)N.T.N.T.
 O-18775% (30)Stim at 30N.T.N.T.
1-Substituent
 O-125373% (30)Stim at 1, 3, 10, and 3050% (10)89% (0.1)
 O-125429% (30)Stim at 3, 10, and 3013% (30)Stim at 10
 O-1255None (3, 10, and 30)20% (10)None (10)65% (10)
 O-130054% (30)Stim at 30N.T.N.T.
4- and/or 5-Substituent
 O-13022% (10)26% (3)107% (30)74% (0.3)
 O-1559118% (30)Stim at 3, 10, and 30N.T.N.T.
 O-169018% (30)24% (10)39% (10)88% (0.3)
 O-169166% (1)15% (3)150% (3)91% (0.1)
 O-170457% (1)19% (30)49% (10)85% (0.3)
 O-17104% (1)42% (10)None (0.3, 1, 3, and 10)82% (10)

Maximum (max) % stimulation (stim) and % inhibition (inhibit) produced by pyrazole analogs tested alone (left) and tested in combination with 3 mg/kg Δ9-THC (right). Dose(s) (mg/kg) at which the effect occurred are given in parentheses.

  • N.T., not tested.