Morphine metabolism, transport and brain disposition

被引：115
作者：
De Gregori, Simona [1 ]
De Gregori, Manuela [2 ,3 ]
Ranzani, Guglielmina Nadia [3 ]
Allegri, Massimo [2 ,4 ]
Minella, Cristina [2 ]
Regazzi, Mario [1 ]
机构：
[1] Fdn IRCCS Policlin San Matteo, Clin Pharmacokinet Unit Transplantat & Autoimmune, I-7100 Pavia, Italy
[2] Fdn IRCCS Policlin San Matteo, Anesthesia Intens Care & Pain Therapy Serv, Pavia, Italy
[3] Univ Pavia, Dept Genet & Microbiol, I-27100 Pavia, Italy
[4] Univ Pavia, Sect Anaesthesiol Resuscitat & Pain Therapy, Dept Surg Sci Resuscitat Rehabil & Organ Transpla, I-27100 Pavia, Italy
来源：
METABOLIC BRAIN DISEASE | 2012年 / 27卷 / 01期
关键词：
Blood-Brain-Barrier; Genetic variability; Morphine; Morphine-3-glucuronide; Morphine-6-glucuronide; Transport mechanisms; OPIOID RECEPTOR; P-GLYCOPROTEIN; BARRIER TRANSPORT; MORPHINE-6-GLUCURONIDE; GENE; RATS; GLUCURONIDATION; POLYMORPHISMS; MICE; MORPHINE-3-GLUCURONIDE;
D O I：
10.1007/s11011-011-9274-6
中图分类号：
R5 [内科学];
学科分类号：
1002 ; 100201 ;
摘要：
The chemical structures of morphine and its metabolites are closely related to the clinical effects of drugs (analgesia and side-effects) and to their capability to cross the Blood Brain Barrier (BBB). Morphine-6-glucuronide (M6G) and Morphine-3-glucuronide (M3G) are both highly hydrophilic, but only M6G can penetrate the BBB; accordingly, M6G is considered a more attractive analgesic than the parent drug and the M3G. Several hypotheses have been made to explain these differences. In this review we will discuss recent advances in the field, considering brain disposition of M6G, UDP-glucoronosyltransferases (UGT) involved in morphine metabolism, UGT interindividual variability and transport proteins.
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页码：1 / 5
页数：5
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