Pasternak G W, Bodnar R J, Clark J A, Inturrisi C E
Cotzias Laboratory of Neuro-Oncology, Memorial Sloan-Kettering Cancer Center, New York, NY.
Life Sci. 1987 Dec 28;41(26):2845-9. doi: 10.1016/0024-3205(87)90431-0.
The 3- and the 6-glucuronides of morphine have been examined in binding studies and in vivo. The 3-glucuronide had poor affinity in all binding studies whereas the 6-glucuronide potently labeled mu, but not delta or kappa receptors with affinities similar to morphine. Microinjections of the 3-glucuronide directly into the periaqueductal gray were without effect. The 6-glucuronide, on the other hand, was up to 20-fold more potent than morphine following microinjections in the same region. High doses of the 6-glucuronide produced profound seizure activity. All 6-glucuronide actions were sensitive to the opiate antagonist naloxone.
吗啡的3-葡萄糖醛酸苷和6-葡萄糖醛酸苷已在结合研究和体内实验中得到检验。在所有结合研究中，3-葡萄糖醛酸苷的亲和力都很差，而6-葡萄糖醛酸苷能有效地标记μ受体，但不能标记δ或κ受体，其亲和力与吗啡相似。将3-葡萄糖醛酸苷直接微量注射到中脑导水管周围灰质中没有效果。另一方面，在同一区域进行微量注射后，6-葡萄糖醛酸苷的效力比吗啡高20倍。高剂量的6-葡萄糖醛酸苷会产生严重的癫痫活动。6-葡萄糖醛酸苷的所有作用都对阿片类拮抗剂纳洛酮敏感。
