. Author manuscript; available in PMC: 2011 Nov 1.

Published in final edited form as: Drug Dev Res. 2010 Nov 1;71(7):404–411. doi: 10.1002/ddr.20388

TABLE 1.

Binding Affinity of Various Ligands to CB1 Receptors With Mutations in Positions 268–271 in EC2


	K_i (nM)
Receptor	SLV319	AVE1625	NESS0327	O-2050	BAY593074	WIN55212-2
WT	1.8 (1.2–2.6)	0.64 (0.37–1.1)	4.6 (3.2–6.5)	3.4 (2.6–4.6)	249 (140–445)	510 (395–658)
F268W	2.0 (1.5–2.5)	2.2 (1.7–2.7)^*	21.0 (18.3–24.2)^*	148 (87.4–251)^*	1857 (841–4101)^*	1829 (1296–2579)^*
[WT:F268W]^a	[1:1]	[1:3]	[1:5]	[1:44]	[1:7]	[1:4]
P269A	2.1 (1.7–2.7)	0.88 (0.70–1.1)	3.0 (2.7–3.4)	68.6 (48.5–97.1)^*	341 (275–422)	2030 (1193–3455)^*
[WT:P269A]^a	[1:1]	[1:1]	[1:1]	[1:20]	[1:1]	[1:4]
H270A	4.0 (2.8–5.8)^*	1.2 (0.89–1.7)^*	6.1 (5.2–7.3)	40.2 (28.7–56.1)^*	412 (348–487)	1999 (1609–2484)^*
[WT:H270A]^a	[1:2]	[1:2]	[1:1]	[1:12]	[1:2]	[1:4]
I271A	8.6 (7.4–10.1)^*	1.8 (1.4–2.3)^*	11.2 (9.8–12.9)^*	166 (119–229)^*	2872 (1543–5348)^*	2825 (2516–3173)^*
[WT:I271A]^a	[1:5]	[1:3]	[1:2]	[1:49]	[1:12]	[1:6]

Data are the median and corresponding 95% confidence limits of three independent experiments performed in duplicate. K_i values for each ligand were determined using 4 nM [³H]SR141716A.

Statistically significant differences from wild-type (P<0.05) using analysis of variance followed by Dunn's post hoc test.

Values represent the K_i ratio for WT to EC2 mutant receptors for the specified compound.