. Author manuscript; available in PMC: 2014 Nov 1.

Published in final edited form as: Eur J Med Chem. 2013 Sep 29;69:881–907. doi: 10.1016/j.ejmech.2013.09.038

Table 6.

Determination of potency (EC₅₀) and maximal stimulation (E_max) on hCB1 and hCB2 receptors of selected compounds^a

Compound	GTPγ[³⁵S] functional assays^a
	Human CB1		Human CB2
	EC₅₀ (nM)	E_max (%)	EC₅₀ (nM)	E_max (%)
CP55,940	N.D.	N.D.	4.13	100
4	96.9 ± 11.9^b	73.6^b	10.5 ± 1.8^b	30.8^b
64	N.A.	N.A.	7.3± 6.7	59.6
81	118.3 ± 4^b	30.4^b	9.8 ± 0.3^b	−76.4^b

CB1 and CB2 assay data are presented as the mean of two determinations. Assay reproducibility was monitored by the use of the reference compound CP55,940. For replicate determinations, the maximum variability tolerated in the test was 20% around the average of the replicates. Efficacies (E_max) for CB1 or CB2 are expressed as a percentage relative to the efficacy of compound CP55,940. N.D. = not determined; N.A.: not active at 1 μM;

from ref [7].