Table 2.

Opioid Agonist or Antagonist activities of Bcp¹- and Dbcp¹-Analogues of TIPP peptides^a

		MVD		GPI
No.	Peptide	IC50 (nM)	Keδ (nM)	IC50 (nM)		Keμ (nM)
1	H-Bcp-Tic-Phe-Phe-OH	3.42 ± 0.36		223 ± 37 (IC40)b
2	H-Bcp-Tic-Phe-OH		18.7 ± 1.2	458 ± 73 (IC35)b
3	H-Bcp-Tic-OH		17.8 ± 0.7			5380 ± 380
4	H-Bcp-TicΨ[CH2NH]Phe-Phe-OH	11.8 ± 1.6 (IC40)b		1460 ± 310 (IC40)b
5	H-Bcp-TicΨ[CH2NH]Cha-Phe-OH	32.0 ± 8.2 (IC40)b		721 ± 78 (IC35)b
6	H-Dbcp-Tic-Phe-Phe-OH		3.07 ± 0.51			373 ± 71
7	H-Dbcp-Tic-OH		1.76 ± 0.30			2910 ± 570
8	H-Tyr-Tic-Phe-Phe-OH (TIPP)c		4.80 ± 0.20	> 10000
9	H-Tyr-Tic-OH		263 ± 40		inactive
10	H-Dmt-Tic-Phe-Phe-OHc		0.196 ± 0.035	769 ± 142
11	H-Dmt-Tic-OHc		6.55 ± 0.27		inactive
12	H-Cdp-Tic-Phe-Phe-OH		0.627 ± 0.058			3070 ± 260

^aValues represent means of 3–6 determinations.

^bPartial agonist.

^cData taken from Schiller et al.10