[Pharmacologically active polymers. 9th communication: retard forms of morphine antagonists (author's transl)].
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.
D000818:Animals; D001575:Benzomorphans / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D003692:Delayed-Action Preparations; D007928:Lethal Dose 50; D051379:Mice; D009019:Morphinans / Q000138:chemical synthesis*; D009020:Morphine / Q000037:antagonists & inhibitors*; D011108:Polymers / Q000138:chemical synthesis* / Q000494:pharmacology
D001575:Benzomorphans; D003692:Delayed-Action Preparations; D009019:Morphinans; D011108:Polymers; D009020:Morphine
Pharmakologisch aktive polymere. 9. Mitt.: Depotformen eines Morphinantagonisten.