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US 5,352,680 AGranted
Delta opioid receptor antagonists to block opioid agonist tolerance and dependence
AssigneeRegents of the University of Minnesota
InventorsPhilip S. Portoghese, Akira E. Takemori
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Abstract
A motion provided to alleviate the tolerance to, or dependence on, an opiate analgesic, by the administration of an effective amount of a selective delta opioid receptor antagonist to a human patient in need of such treatment.
Claims23
A therapeutic method for treating opiate tolerance in a human undergoing opiate administration comprising administering to said human in need of such treatment an amount of a delta opioid receptor antagonist of the formula I:
- ##STR8## wherein R.sup.1 is (C.sub.1 -C.sub.5)alkyl, C.sub.3 -C.sub.6 (cycloalkyl)alkyl, C.sub.5 -C.sub.7 (cycloalkenyl)alkyl, aryl, aralkyl, trans(C.sub.4 -C.sub.5)alkenyl, allyl or furan-2-ylalkyl, R.sup.2 is H, OH or O.sub.2 C(C.sub.1 -C.sub.5)alkyl;
- R.sup.3 is H, (C.sub.1 -C.sub.5)alkyl;
- or ((C.sub.1 -C.sub.5)alkyl)CO;
- X is O, S or NY, wherein Y is H or (C.sub.1 -C.sub.5)alkyl;
- and R.sup.4 and R.sup.5 are individually H, F, Cl, Br, NCS, NO.sub.2, NH.sub.2, (C.sub.1 -C.sub.5)alkyl or (C.sub.1 -C.sub.5)alkoxy, or together are benzo;
- and the pharmaceutically acceptable salts thereof;
- wherein said amount is effective to block or reduce the tolerance of said human to an opioid mu receptor agonist.
4 more elements
Dependencies are inferred from the claim text.