. Author manuscript; available in PMC: 2009 Sep 25.

Published in final edited form as: J Med Chem. 2008 Sep 25;51(18):5866–5870. doi: 10.1021/jm8004702

Table 1.

Angatonist Potencies (K_e values) of (2S)-Mdcp¹ - and (2S)-Mdp¹ -Analogues of Opioid Peptides^a

		GPI	GPI	MVD	K_e ratio
no.	antagonist	K_e^μ (nM)^b	K_e^κ (nM)^c	K_e^δ (nM)^d	μ/δ/κ	δ/μ/κ
1	(2S)-Mdcp-c[D-Cys-Gly-Phe(pNO₂)-D-Cys]NH₂	1.24 ± 0.23	18.9 ± 0.3	9.78 ± 1.16	1/8/15
2	(2S)-Mdp-c[D-Cys-Gly-Phe(pNO₂)-D-Cys]NH₂^e	1.48 ± 0.18	6.41 ± 0.18	3.48 ± 0.28	1/2/4
3	(2S)-Mdcp-c[D-Pen-Gly-Phe(pF)-Pen]-Phe-OH	1170 ± 100	9980 ± 1650	0.326 ± 0.030		1/3590/30600
4	(2S)-Mdp-c[D-Pen-Gly-Phe(pF)-Pen]-Phe-OH^f	668 ± 40	4370 ± 860	0.785 ± 0.135		1/851/5570
5	[(2S)-Mdcp¹]Dyn A(1-11)-NH₂	401 ± 62	5.96 ± 0.80	843 ± 88	1/2/0.015
6	[(2S)-Mdp¹]Dyn A(1-11)-NH₂^g	925 ± 94	3.92 ± 0.65	3320 ± 520	1/4/0.004

Values represent means of three to six determinations.

Determined with TAPP as μ agonist.

Determined with U50,488 as κ agonist.

Determined with DPDPE as δ agonist.

Data taken from Schiller et al.²

Data taken from Schiller et al.⁴

Data taken from Lu et al.³