. Author manuscript; available in PMC: 2009 May 7.

Published in final edited form as: J Med Chem. 2007 Oct 10;50(22):5528–5532. doi: 10.1021/jm061465o

Table 2.

Bioactivities of the Opioid Ligands

no	hDOR^a [³H]DPDPE ^b		rMOR^a [³H]DAMGO^c		[³⁵S]GTP-γ-S binding						IC₅₀ (nM)^e

					hDOR^d			rMOR^d

	LogIC₅₀^f^,^g	Ki^h (nM)	LogIC₅₀^f^,^g	Ki^h (nM)	LogEC₅₀^f	EC₅₀ (nM)ⁱ	Emax^j (%)	LogEC₅₀^f	EC₅₀ (nM)ⁱ	Emax^j (%)	MVD(δ)	GPI(μ)
8	-4.70±0.17	9400	-4.93±0.20	5400	ns	ns	ns	ns	ns	ns	1%	0%
10	-7.51±0.12	14	-7.52±0.26	14	-6.29±0.15	510	92	-6.90±0.31	125	53	380±80	160±50
11	-8.12±0.11	3.7	-8.60±0.08	1.2	-7.54±0.09	29	78	-7.79±0.09	16	52	250±50	47±12
12	-7.88±0.12	6.1	-8.63±0.16	1.1	-6.95±0.10	110	32	-7.96±0.14	11	52	290±70	95±6
13	-4.87±0.23	7000	-4.96±0.31	5700	Ns	ns	ns	Ns	ns	ns	3%	3%
14	-8.75±0.08	0.69	-7.24±0.24	23	-7.43±0.39	37	72	-7.39±0.41	41	63	24±2	200±60
15	-6.40±0.19	180	-7.05±0.07	40	-6.78±0.20	170	15	-7.08±0.29	82	32	10%	15%
16	-9.10±0.10	0.36	-9.08±0.22	0.38	-9.12±0.17	0.77	24	-9.05±0.18	0.88	50	1.8±0.2	8.5±3.3
17	-8.18±0.08	3.2	-7.92±0.06	5.7	-6.82±0.20	150	71	-7.63±0.25	24	43	250±70	120±50
DAMGO	-	-	-	-	-	-	-	-7.44±0.19	37	150	-	-
DPDPE	-	-	-	-	8.80±0.25	1.6	69
YDAGF-NH₂	-6.14±0.16	300	-8.24±0.13	2.8	-6.72±0.17	190	44	-7.98±0.22	13	99	120±10	47±10
DALEA²⁰-²¹	-	2.4	-	7.7	-	-	-	-	-	-	7.6	8.3

Competition analyses were carried out using membrane preparations from transfected HN9.10 cells that constitutively expressed the respective receptor types.

K_d = 0.50 ± 0.1 nM.

K_d = 0.85 ± 0.2 nM.

Expressed from CHO cell.

Concentration at 50% inhibition of muscle contraction at electrically stimulated isolated tissues.

Logarithmic values determined from the non-linear regression analysis of data collected from at least two independent experiments.

Competition against radiolabeled ligand.

Antilogarithmic value of the respective IC₅₀.

ⁱ

Antilogarithmic value of the respective EC₅₀.

Net total bound/basal binding × 100 ± SEM.

ns: not saturated