Enkephalin analogs

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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Details

514 9, 514 11, 530317, 530330, A61K 3702, C07K 512, C07K 706

Patent

active

053267516

ABSTRACT:
A new class of opioid receptor analogs is described based on an alanine substitution in the three position in the enkephalin analog DPDPE. The alanine-substituted analogs show increased selectivity for the delta type of opioid receptors over the mu type of receptors.

REFERENCES:
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patent: 4684620 (1987-09-01), Hruby et al.
patent: 5061691 (1991-10-01), Yagi et al.
Toth, G. et al., "[D-Pen.sup.2, D-Pen.sup.5 ]enkephalin Analogues With Inased Affinity and Selectivity for Opioid Receptors," J. Med. Chem. 33:249-253 (1990).
Hruby, V. J. and C. A. Gehrig, "Recent Developments in the Design of Receptor Specific Opioid Peptides," Medicinal Research Reviews 9:3:343-401 (1989).
Clark, J. A., et al., "[D-Pen.sup.2, D-Pen.sup.5 ]enkephalin (DPDPE): A .delta.-selective Enkephalin with Low Affinity for .mu.1 Opiate Binding Sites," E. J. Pharm. 128:303-304 (1986).
Haaseth, R. C. et al., "Potent and Selective 3-position Analogs of DPDPE," INRC/CPDD Meeting Jun. 20-27, 1992 (Poster presented Jun. 27).
Misika, A. et al., "Computer Modeling of Opioid Selective Ligands: Possible New Topographical Relationships to Bioactivity are Examined with New Analogs Designed for .delta. Opioid Receptor," Peptides (J. Smith and J. Rivier Eds., Escom. 1991).

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