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The binding of alkylendiamide dimers of the three N-terminal residues of [D-Ala2,D-Leu5]enkephalin (DADL) to rat brain and Ng108-15 neuroblastoma-glioma cell membranes was compared with that of DADL, Tyr-D-Ala-Gly-NMe-Phe-Gly-ol (DAGO) and morphiceptin. Tritiated DADL and DAGO were used as labeled ligands for delta- and mu-receptors, respectively. Dimerization of the tripeptides resulted in dramatic increases in both mu and delta binding. The binding to mu-receptors showed two peaks at an alkyl chain length of n = 2 and approximately n = 16. In contrast, delta binding (NG108-15 cells) increased steadily with increasing chain length. The dimers with n less than 18 were mu-preferential, and the one with n = 2 showed the most dramatic increase in mu selectivity with a 400 fold higher affinity to mu- than to delta-receptors. For long-chain alkyl spacers the compounds became delta selective.
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
February 1981,
Biulleten' eksperimental'noi biologii i meditsiny,
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
December 1988,
Endocrinologia experimentalis,
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
October 1978,
Life sciences,
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
April 1990,
Journal of neurochemistry,
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
September 2003,
Peptides,
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
January 1986,
Experimental and clinical immunogenetics,
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
September 1985,
FEBS letters,
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
April 1994,
International journal of peptide and protein research,
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
October 1988,
Neuropeptides,
R A Lutz, and
R A Cruciani, and
Y Shimohigashi, and
T Costa, and
S Kassis, and
P J Munson, and
D Rodbard
January 1986,
NIDA research monograph,
