Lipidic Peptides. Ill: Lipidic Amino Acid and Oligomer Conjugates of Morphine
作者:R.A. Hughes、I. Toth、P. Ward、S.J. Ireland、W.A. Gibbons
DOI:10.1002/jps.2600801202
日期:1991.12
A series of lipidic morphine esters 1b-1f with enhanced membrane-like character were synthesized by coupling the lipidic amino acids 2a-2e to the phenolic hydroxyl group of the opioid analgesic morphine (1a). The antinocioceptive activity of the esters 1b-1f was determined in vivo following both iv and oral dosing. After iv administration, four of the conjugates, 1b, 1c, 1d, and 1f, exhibited antinocioceptive
通过将脂质氨基酸2a-2e与阿片类镇痛吗啡(1a)的酚羟基偶联,合成了一系列具有增强的膜样特性的脂质吗啡酯1b-1f。在静脉内和口服给药后,在体内确定了酯1b-1f的抗伤害感受活性。静脉内给药后,四种缀合物1b,1c,1d和1f在小鼠腹部收缩试验中显示出抗伤害感受活性,其效力与母体化合物1a相似。结合物1b在口服给药后表现出活性。