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A number of studies reported striking differences in antinociceptive responses to morphine as a function of sex. Although sex differences in the sensitivity to morphine are widely characterized in rodents, the underlying causes are not identified. Gonadal steroids are believed to contribute to sex differences in response to opioid-induced antinociception. In rats, morphine is metabolized by glucuronidation...
Using heterologous expression in Xenopus laevis oocytes, we compared the potencies of morphine, morphine-6β-glucuronide (M6G), and morphine-3-glucuronide (M3G) for cloned human μ- (hMOR), κ- (hKOR), and δ-opioid receptors (hDOR). Each receptor subtype was individually co-expressed with heteromultimeric G-protein coupled inwardly rectifying K + (GIRK) channels, consisting of GIRK1 and GIRK2...
Morphine-3-glucuronide (M3G) and morphine-6-glucuronide (M6G) are active metabolites of morphine. The effects of M3G and M6G on the opioid receptor transduction system has not yet been fully elucidated. Formation of cAMP after treatment with various doses of morphine, M3G, and M6G was studied. M6G and morphine, but not M3G, showed a dose dependent inhibition of cAMP accumulation. Naloxone blocked...
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