. Author manuscript; available in PMC: 2014 Oct 2.

Published in final edited form as: J Med Chem. 2008 Sep 25;51(18):5608–5616. doi: 10.1021/jm800329z

Table 1.

IC₅₀ and K_i values for the CBL₁ and CB₂ receptors and cLogP data for ligands 2, (-)-12a, (+)-12a, (-)-12c and (+)-12c. graphic file with name nihms-58026-t0010.jpg

Ligand	R¹	CB₁ IC₅₀ (nM)^a	CB₂ IC₅₀ (nM)^a	CB₁ K_i (nM)^a	CB₂ K_i (nM)^a	cLogP^b
2		2.2 ± 0.5	4,570 ± 410	0.4 ± 0.1	697 ± 63	6.95
(-)-12a	CN	2.8 ± 0.3	> 33,000	0.5 ± 0.1	> 5,000	3.85
(+)-12a	CN	100 ± 10	> 33,000	16.9 ± 2.0	> 5,000	3.85
(-)-12c	I	1.9 ± 0.7	> 33,000	0.3 ± 0.1	> 5,000	5.07
(+)-12c	I	103.5 ± 9.0	> 33,000	17.4 ± 2.0	> 5000	5.07

Values are represent the mean ± SD of three determinations.

cLogP values were calculated by using the Pallas 3.0 software (Compudrug, USA).