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. Author manuscript; available in PMC: 2012 May 22.

Published in final edited form as: J Med Chem. 2007 Apr 4;50(9):2254–2258. doi: 10.1021/jm061327z

Table 1.

Ki Values for the Inhibition of μ, δ and κ Opioid Binding to Chinese Hamster Ovary Membrane by Hetero-dimeric Opioids

compd	Ki ± SEM (nM)			Selectivity
	[³H]DAMGO(μ)	[³H]U69,593(κ)	[³H]Naltrindole(δ)	κ/μ	κ/δ
1 (Butorphan)	0.23 ± 0.01	0.079 ± 0.003	5.9 ± 0.6	3	70
2 (Nalbuphine)	0.89 ± 0.02	2.2 ± 0.01	240 ± 18	0.4	109
3 (Naltrexone)	0.23 ± 0.05	0.25 ± 0.02	38 ± 3	1	152
4 (Naloxone)	0.79 ± 0.02	1.1 ± 0.03	76 ± 2	1	69
5^a	0.71 ± 0.02	0.29 ± 0.02	18 ± 1	2	62
6	0.46 ± 0.02	0.34 ± 0.008	28 ± 4	1	82
7	0.29 ± 0.0007	0.12 ± 0.002	15 ± 2	2	125
8	0.43 ± 0.001	0.13 ± 0.002	39 ± 6	3	300
9^a	0.09 ± 0.004	0.05 ± 0.001	4.2 ± 0.4	2	84

^a

These compounds were reported as compounds (8) and (18) in ref. 17