ANALGESIC POTENCIES OF MORPHINE 3-SULFATES AND 6-SULFATES AFTER INTRACEREBROVENTRICULAR ADMINISTRATION IN MICE - RELATIONSHIP TO STRUCTURAL CHARACTERISTICS DEFINED BY MASS-SPECTROMETRY AND NUCLEAR MAGNETIC-RESONANCE
ANALGESIC POTENCIES OF MORPHINE 3-SULFATES AND 6-SULFATES AFTER INTRACEREBROVENTRICULAR ADMINISTRATION IN MICE - RELATIONSHIP TO STRUCTURAL CHARACTERISTICS DEFINED BY MASS-SPECTROMETRY AND NUCLEAR MAGNETIC-RESONANCE
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DOI：
10.1002/jps.2600740804
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发表时间：
1985-01-01
影响因子：
3.8
通讯作者：
FUJIMOTO, JM
中科院分区：
文献类型：
--
作者：
BROWN, CE;ROERIG, SC;FUJIMOTO, JM
3-硫酸吗啡与吗啡一样，在3位携带极性酸性基团，在脑室内给药后，其镇痛效力与吗啡相差不大。这与非电离的3-甲基醚和3-甲基醚不同，它们是比吗啡更弱的镇痛药。硫酸吗啡6与吗啡的不同之处在于其在生理pH值上具有碳-6电离基团，在脑室内给药后比吗啡具有更强的镇痛作用。羟基修饰后镇痛效力的变化似乎只反映了点电荷的改变，而不是结构的改变。
Morphine 3-sulfate, which carries a polar, acidic group at the 3-position much like morphine, does not differ greatly in analgesic potency from morphine following intracerebroventricular administration. This differs from the non-ionizable 3-methyl and 3-methyl ethers, which are less potent analgesics than morphine. Morphine 6-sulfate, which differs from morphine by having an ionizable group at carbon-6 at physiological pH, is a more potent analgesic than morphine following intracerebroventricular administration. Variations in analgesic potency following modifications at the hydroxyl groups appear only to reflect alterations in point charges rather than structural alterations.