Skip to main content

View full-text article in PMC

. Author manuscript; available in PMC: 2015 Jan 3.

Published in final edited form as: Expert Opin Investig Drugs. 2013 Dec 13;23(2):227–241. doi: 10.1517/13543784.2014.856879

Table 1.

Pharmacological data of Dicarba analogs of H-Tyr-c[D-Cys-Phe-L(or D)-Cys]-NH₂ and H-Tyr-c[D-Cys-Gly-Phe-L(or D)-Cys]-NH₂ at opioid receptors (OR).


Compound number	GPI	MVD	GPI/MVD	OR binding affinity			Binding ratio

	IC₅₀ (nM)	IC₅₀ (nM)	IC₅₀ ratio	K_i^μ (nM)	K_i^δ (nM)	K_i^κ (nM)	K_i^μ/K_i^δ/K_i^κ
1	436	460	1/1.06	–	–	–	–
2	162	444	1/2.74	–	–	–	–
3	76.5	655	1/8.56	–	–	–	–
4	64.7	740	1/11.4	11.0	373	–	1/34/–
5	176	246	1/1.40	–	–	–	–
6	208	786	1/3.78	–	–	–	–
7	20.0	28.8	1/1.44	–	–	–	–
8	1.81	0.496	3.65/1	2.4	6.55	200	1/3/83
9	0.898	0.275	3.27:1	0.616	1.25	57.6	1/2/94
10	1.02	3.19	1/3.12	2.34	5.87	309	1/3/132
11	1.65	0.603	2.74/1	1.74	1.61	40.1	1/1/23
12	11.9	9.91	1.2/1	2.27	7.04	498	1/3/219
13	5.63	4.38	1.3/1	1.05	1.92	30.4	1/2/29
14	11.2	3.64	3.1/1	1.17	3.34	71.5	1/3/61
15	1.30	0.562	2.31/1	0.550	0.822	44.9	1/1/82