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. Author manuscript; available in PMC: 2010 Nov 12.

Published in final edited form as: J Med Chem. 2009 Nov 12;52(21):6941–6945. doi: 10.1021/jm9004913

Table 1.

Opioid Receptor Binding Affinities of Bcp¹- and Dbcp¹-Analogues of TIPP peptides^a

....					K_i ratio
No.	Peptide	K_i^δ (nM)	K_i^μ (nM)	K_i^κ (nM)	δ/μ/κ
1	H-Bcp-Tic-Phe-Phe-OH	0.605 ± 0.058	87.7 ± 8.0	270 ± 74	1/145/446
2	H-Bcp-Tic-Phe-OH	0.536 ± 0.057	173 ± 10	1580 ± 720	1/323/2950
3	H-Bcp-Tic-OH	0.646 ± 0.088	2270 ± 210	4760 ± 200	1/3510/7370
4	H-Bcp-TicΨ[CH₂NH]Phe-Phe-OH	2.00 ± 0.19	323 ± 16	1240 ± 50	1/162/620
5	H-Bcp-TicΨ[CH₂NH]Cha-Phe-OH	3.31 ± 0.32	334 ± 64	1660 ± 60	1/101/502
6	H-Dbcp-Tic-Phe-Phe-OH	0.783 ± 0.046	142 ± 41	597 ± 73	1/181/762
7	H-Dbcp-Tic-OH	0.825 ± 0.107	615 ± 31	2750 ± 70	1/745/3330
8	H-Tyr-Tic-Phe-Phe-OH (TIPP)^b	1.22 ± 0.07	1720 ± 50	> 1000	1/1410/>820
9	H-Tyr-Tic-OH	242 ± 28	> 1000	> 10000	-
10	H-Dmt-Tic-Phe-Phe-OH^b	0.248 ± 0.046	141 ± 24	> 1000	1/569/>4030
11	H-Dmt-Tic-OH^b	1.84 ± 0.24	1360 ± 160	> 1000	1/739/>543
12	H-Cdp-Tic-Phe-Phe-OH	0.501 ± 0.060	2210 ± 490	> 1000	1/4410/>2000

^a

Values represent means of 3–6 determinations.

^b

Data taken form Schiller et al.10