1973 年 93 巻 10 号 p. 1302-1307
In connection with our previous findings that morphine 6-glucuronide and morphine 6-sulfate, although highly polar conjugates, induced potent analgesia, synthesis and analgesic effect of morphine 3-and 6-phosphate were investigated. Chemical synthesis of these phosphate esters was accomplished by utilizing cyanoethylphosphate as a phosphorylation reagent. Analgesic effect of both compounds in mice were found to be about the same order of magnitude as that of morphine when injected subcutaneously or intracerebrally. The tonic extensor convulsion was also observed in mice when morphine phosphate esters were injected intracerebrally (100 μg/body).