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• W2078346327 abstract "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 subunits, and RGS4, a regulator of G-protein signaling. The two-microelectrode voltage clamp technique was used to measure the opioid receptor-activated GIRK1/GIRK2 channel responses. Compared with morphine, M6G had higher potency at the hMOR, lower potency at the hKOR, and similar potency at the hDOR, while M3G showed a 1000-fold lower and non-selective potency via opioid receptors. In contrast to naloxone, M3G did not antagonize the effects of morphine at the hMOR. We also investigated whether Trp318 and His319 provide the molecular basis for μ/δ selectivity and μ/κ selectivity of morphinan alkaloids by mutating these residues to their corresponding residues in κ- and δ-opioid receptors. A single-point mutation (W318L) on hMOR completely conferred δ-like potency for morphine and M6G on the mutant μ-receptor. Double mutation at Trp318 and His319 positions (Trp318Y/His319Y) only partially conferred κ-like potency for morphine and M6G; the decrease in potency for M6G was significantly larger than for morphine. The results of our study show that both M6G and M3G are opioid receptor agonists with different potencies and that the potency of morphinan receptor ligands can be changed by selective mutations of hMOR at the Trp318 and His319 positions." @default.
• W2078346327 created "2016-06-24" @default.
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• W2078346327 date "2001-11-01" @default.
• W2078346327 modified "2023-10-03" @default.
• W2078346327 title "Morphine-6β-glucuronide and morphine-3-glucuronide, opioid receptor agonists with different potencies11Abbreviations: M3G, morphine-3-glucuronide; M6G, morphine-6β-glucuronide; MOR, μ-opioid receptor; KOR, κ-opioid receptor; DOR, δ-opioid receptor; GIRK channel, G-protein coupled inwardly rectifying K+ channel; RGS, regulator of G-protein signaling; GAP, GTPase-activating protein; TM, transmembrane domain, and HK, high potassium." @default.
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• W2078346327 doi "https://doi.org/10.1016/s0006-2952(01)00761-4" @default.
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