2^′, 6^′-Dimethylphenylalanine : A Useful Aromatic Amino Acid Surrogate for Tyr or Phe Residue in Opioid Peptides

Table 2

𝐾_e values of opioid receptor antagonists against Dmp-containing YRFB analogs in the GPI and MVD assays.

Peptides		𝐾e (nM)
	GPI	MVD
	CTAP	CTAP	N,N(Me)2Dmt-Tic-OH
[Dmp^3]YRFB (22)	22.7	11.4	>1000
[Dmp^1]YRFB (24)	25.1	13.4	>1000
[Dmp^1,3]YRFB (25)	21.3	10.2	>1000
YRFB	26.8	21.2	>1000
[Dmt^1]YRFB^b	85.5	7.89	192
DT	NT^a	>1000	0.64

^aNot tested.