Bis-penicillamine enkephalins possess highly improved specificity toward delta opioid receptors.

HI Mosberg, R Hurst, VJ Hruby, K Gee… - Proceedings of the …, 1983 - National Acad Sciences
The conformationally restricted, cyclic, disulfide-containing, enkephalin analogs [2-D-
penicillamine, 5-L-penicillamine] enkephalin [(D-Pen2, L-Pen5] enkephalin) and [2-D …

Conformationally constrained cyclic enkephalin analogs with pronounced delta opioid receptor agonist selectivity

HI Mosberg, R Hurst, VJ Hruby, JJ Galligan, TF Burks… - Life Sciences, 1983 - Elsevier
The enkephalin analogs,[D-Pen 2, L-Cys 5]-and [D-Pen 2, D-Cys 5]-enkephalin are cyclic
compounds, conformationally constrained by virtue of their 14-membered, disulfide …

Characterization of [3H][2-D-penicillamine, 5-D-penicillamine]-enkephalin binding to delta opiate receptors in the rat brain and neuroblastoma--glioma hybrid cell line …

K Akiyama, KW Gee, HI Mosberg… - Proceedings of the …, 1985 - National Acad Sciences
Specific binding properties of the tritium-labeled delta opiate receptor agonist [3H][2-D-
penicillamine, 5-D-penicillamine] enkephalin [(3H][D-Pen2, D-Pen5] enkephalin) were …

Dehydro-enkephalins. IV. Discriminative recognition of delta and mu opiate receptors by enkephalin analogs

Y Shimohigashi, ML English, CH Stammer… - Biochemical and …, 1982 - Elsevier
We have studied the receptor binding activities of C-terminal free and amidated enkephalins
with and without the dehydrophenylalanine 4 residue. For the selective labeling of so-called …

[HTML][HTML] A single residue, aspartic acid 95, in the delta opioid receptor specifies selective high affinity agonist binding.

H Kong, K Raynor, K Yasuda, ST Moe… - Journal of Biological …, 1993 - Elsevier
The enkephalins, dynorphins, and endorphins are endogenous opioids which function as
neurotransmitters, neuromodulators, and hormones and are involved in the perception of …

Topographically designed analogs of [cyclic][D-Pen2, D-Pen5] enkephalin

VJ Hruby, G Toth, CA Gehrig, LF Kao… - Journal of medicinal …, 1991 - ACS Publications
Introduction There is now overwhelming evidence from pharmacological considerations2" 4
and fromstructure-activity studies5 that the endogenous opioid peptides methionine …

[HTML][HTML] Affinity labeling of delta-opiate receptors using [D-Ala2, Leu5, Cys6] enkephalin. Covalent attachment via thiol-disulfide exchange.

WD Bowen, SB Hellewell, M Kelemen, R Huey… - Journal of Biological …, 1987 - Elsevier
[D-Ala2, Leu5, Cys6] Enkephalin (DALCE) is a synthetic enkephalin analog which contains
a sulfhydryl group. DALCE binds with high affinity to delta-receptors, with moderate affinity to …

Deltakephalin, Tyr-D-Thr-Gly-Phe-Leu-Thr: a new highly potent and fully specific agonist for opiate δ-receptors

JM Zajac, G Gacel, F Petit, P Dodey, P Rossignol… - Biochemical and …, 1983 - Elsevier
Abstract Deltakephalin, Tyr-D-Thr-Gly-Phe-Leu-Thr (DTLET) was rationally designed as
pure δ-probe from proposed models of μ and δ opiate receptors. On peripheral organs …

Synthesis and opioid activities of stereoisomers and other D-amino acid analogs of methionine-enkephalin

DH Coy, AJ Kastin, AV Schally, O Morin… - Biochemical and …, 1976 - Elsevier
A series of D-amino acid-substituted analogs of the opiate peptide, methionine 5-
enkephalin, were synthesized by solid-phase methods and tested for their abilities to inhibit …

[HTML][HTML] Location of Regions of the Opioid Receptor Involved in Selective Agonist Binding (∗)

K Fukuda, S Kato, K Mori - Journal of Biological Chemistry, 1995 - ASBMB
To elucidate which portions of the opioid receptor molecules are involved in the ligand
selectivity, we have expressed chimeric receptors between the rat δ-and μ-opioid receptors …