Abstract：
:It has been suggested that morphine-6-glucuronide, a major metabolite of the opioid analgesic morphine, is more potent as an analgesic than the parent drug. This finding appears not to be due to differences in affinity for opioid receptors. Therefore, in the present study the opioid receptor mediated effects of morphine and morphine-6-glucuronide were compared in vitro using electrically induced contractions of isolated guinea-pig ilea in the absence and presence of increasing concentrations of the selective opioid receptor antagonists CTAP (D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2) (mu) and norbinaltorphimine (kappa). The results showed a similar efficacy and potency for morphine and morphine-6-glucuronide and indicated that both compounds act reversibly, mainly at mu-opioid receptors. It is concluded that morphine and its metabolite morphine-6-glucuronide are equipotent at mu-opioid receptors.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Schmidt N,Brune K,Geisslinger Gdoi
10.1016/0014-2999(94)90105-8subject
Has Abstractpub_date
1994-04-01 00:00:00pages
245-7issue
1-3eissn
0014-2999issn
1879-0712pii
0014-2999(94)90105-8journal_volume
255pub_type
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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journal_title：European journal of pharmacology
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abstract：:Whole-cell patch-clamp recordings investigated the electrophysiological effects of 2'-hydroxy-4'-methoxyacetophenone (paeonol), one of the major components of Moutan Cortex, in hippocampal CA1 neurons and nucleus ambiguus (NA) neurons from neonatal rats as well as in lung epithelial H1355 cells expressing Kv2.1 or Kv1...
journal_title：European journal of pharmacology
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