Table 2

Ability of various cannabinoid receptor ligands to stimulate [35S]GTPγS binding in rat cerebellar membranes at a GDP concentration of 100 μM

CompoundEmaxEC50CB1Ki2-i
% Stimulation nM nM
CP 55,244165  (148–183)0.47  (0.22–0.96)0.112-a
WIN 55212-2156  (144–169)151.1  (101.6–227)1.892-b
Deoxy-HU-210150  (95–205)9.60  (0.91–95.6)1.152-c
HU-210140  (117–152)0.55  (0.25–1.20)0.732-d
CP 55,940114  (97–131)17.57  (7.03–43.94)0.582-e
Fluoromethanand- amide97  (55–140)25.37  (4.98–129.2)5.702-e
JWH-03056  (37–76)82.40  (14.0–484.1)872-f
JWH-07329  (19–40)104.8  (16.94–648.3)8.902-g
O-106460  (5–116)246.2  (12.45–4869)0.972-g
AnandamideNANA  892-h
THCNANA40.702-e
CannabinolNANA  3082-e
  • NA, not applicable; no significant concentration-dependent stimulation.

  • 2-a Melvin et al. 1995.

  • 2-b Kuster et al., 1993.

  • 2-c Huffman et al., 1996.

  • 2-d Compton et al., 1993.

  • 2-e Showalter et al., 1996.

  • 2-f Lainton et al., 1995.

  • 2-g B. R. Martin, unpublished results.

  • 2-h Adams et al., 1995.

  • 2-i CB1, central cannabinoid receptor.

  • The numbers in parentheses represent 95% confidence limits.