Batz H G, Daniel H, Franzmann G, Koldehoff J, Merz H, Ringsdorf H, Stockhaus K
Arzneimittelforschung. 1977;27(10):1884-8.
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.
已合成吗啡拮抗剂（--）-α-5,9-二甲基-2-（3-呋喃甲基）-2'-羟基-6,7-苯并吗啡烷的丙烯酰基、甲基丙烯酰基、N-乙烯基甲酰基和甲基丙烯酰基-甘氨酰衍生物。将不同的不饱和衍生物与合适的共聚单体共聚以得到水溶性聚合物。在小鼠身上进行的药理试验表明，与游离拮抗剂相比，作用持续时间增加了2至30倍。拮抗剂与聚合物的结合导致急性毒性降低。
