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US 5,326,751 AGranted
Enkephalin analogs
AssigneeArizona Board of Regents on Behalf of the University of Arizona
InventorsRonald C. Haaseth, Victor J. Hruby
Life of this patent
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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.
Claims17
A polypeptide of the formula:
- ##STR6## wherein R.sup.1 is L-tyrosine, or L-tyrosine with a halogen or methyl substitutions;
- R.sup.2 is D-penicillamine or D-cysteine;
- R.sup.3 is phenylalanine or phenylalanine with one to three same or different halogen, nitro, or methyl substitutions;
- and
- R.sup.4 is D-penicillamine, L-penicillamine, D-cysteine or L-cysteine.
2 more elements
A polypeptide of the formula:
- ##STR7## wherein R.sup.1, R.sup.2, and R.sup.3 are the same or different and are H, F, Cl, Br, I, NO.sub.2, NH.sub.2, or a lower alkyl of less than five carbons.
A pharmaceutical composition comprising an opioid receptor agonist having enhanced specificity for the delta opioid receptors, the agonist having the formula:
- ##STR8## wherein R.sup.1, R.sup.2, and R.sup.3 are the same or different and are H, F, Cl, Br, I, NO.sub.2, NH.sub.2 or a lower alkyl of less than five carbons;
- or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.