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Arzneimittelforschung ; 27(10): 1884-8, 1977.
Article in German | MEDLINE | ID: mdl-579098

ABSTRACT

Acryloyl, methacryloyl, N-vinylcarbamoyl, and methacryloyl-glycyl derivatives of the morphine antagonist (--)-alpha-5,9-dimethyl-2-(3-furylmethyl)-2'-hydroxy-6,7-benzomorphane have been synthesized. The different unsaturated derivatives were copolymerized with appropriate comonomers to yield water-soluble polymers. Pharmacological tests in mice showed a 2--30 fold increase in duration of action in comparison to the free antagonist. The binding of the antagonist to the polymers resulted in a reduced acute toxicity.


Subject(s)
Benzomorphans/chemical synthesis , Morphinans/chemical synthesis , Morphine/antagonists & inhibitors , Polymers/chemical synthesis , Animals , Benzomorphans/analogs & derivatives , Benzomorphans/pharmacology , Delayed-Action Preparations , Lethal Dose 50 , Mice , Polymers/pharmacology
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