Table 1.

Antagonism of agonist stimulated yeast expressing hCB₁ receptors

Compound	100 nM CP55,940 IC50 (nM)	400 nM WIN55212-2 IC50 (nM)	4 μM AEA IC50 (nM)	1.5 μM 2-AG IC50 (nM)
PSNCBAM-1	45.2±7.5	208.7±27.9	37±5.3	230.3±12.2
SR141716A	22.5±7.3	6.5±1.4	16±3.2	11.4±2.9

Abbreviations: AEA, arachidonoyl ethanolamide; PSNCBAM-1, 1-(4-chlorophenyl)-3-[3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl]urea; SR141716A, N-(piperidin-1-yl)-5-(4-cholrophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide.

Potency of PSNCBAM-1 and SR141716A against a range of agonist-stimulated receptor signalling in Saccharomyces cerevisiae stably expressing recombinant human CB₁ receptors. Yeast cells were incubated with compounds at 30°C and reporter gene expression was measured by a fluorescent read-out. Agonist concentrations used were determined by their EC₉₀ values in the assay. Data are mean IC₅₀±s.e.m. from three experiments.