Abstract：
:Morphine 6-glucuronide, a major metabolite of morphine with potent analgesic actions, is a potent inhibitor of intestinal motility when administered to rats by the intracerebroventricular (i.c.v.) route. Morphine 6-glucuronide was 62-fold more active than morphine in inhibiting gastrointestinal transit, whereas it was only 25-fold more potent in abolishing intestinal migrating myoelectric complexes. Pretreatment with naloxone (5 micrograms/rat i.c.v.) completely prevented the disappearance of migrating myoelectric complexes induced by the morphine metabolite. In contrast, in the guinea pig ileum bioassay, morphine 6-glucuronide and morphine inhibited the electrically evoked contractions of the tissue with similar potency, although in the guinea pig ileum binding assay the metabolite showed 4-fold lower affinity for the opiate receptor. The low naloxone Ke values against morphine 6-glucuronide or morphine indicated that the action of both drugs in guinea pig ileum was mediated by mu-opioid receptors.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Massi P,Giagnoni G,Basilico L,Gori E,Rubino T,Parolaro Ddoi
10.1016/0014-2999(94)90201-1subject
Has Abstractpub_date
1994-03-03 00:00:00pages
269-74issue
3eissn
0014-2999issn
1879-0712pii
0014-2999(94)90201-1journal_volume
253pub_type
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