. Author manuscript; available in PMC: 2016 Jan 6.

Published in final edited form as: J Med Chem. 2015 May 7;58(10):4220–4229. doi: 10.1021/acs.jmedchem.5b00007

Table 2. Effect of 2 (10 μM) on Orthosteric Agonist Competition Binding K_i Values in CHO-hDOPr Cell Membranes^a.

ligand	K_i (nM) (95% CI (nM))		affinity ratio (vehicle K_i)/(2 K_i)

	with vehicle	with 2 (10 μM)
leu-enkephalin	221 (119–324)	7(3–12)	32
SNC80	71 (20–122)	5(3–7)	14
TAN67	10 (7–14)	3 (0.2–5.8)	3

2 had no effect on ³H-DPN binding (see Figure 2) but increased the affinity of orthosteric agonist competition binding curves. Data are presented as the mean ± SEM of three experiments.

Table 2. Effect of 2 (10 μM) on Orthosteric Agonist Competition Binding Ki Values in CHO-hDOPr Cell Membranesa.

Table 2. Effect of 2 (10 μM) on Orthosteric Agonist Competition Binding K_i Values in CHO-hDOPr Cell Membranes^a.