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- W2065652085 abstract "Tramadol hydrochloride is a centrally acting synthetic analgesic in widespread clinical use. Despite different degrees of opioid-like characteristics in preclinical tests, it is characterized by lack of full naloxone reversibility or naloxone-precipitated withdrawal in humans. To investigate this apparent discrepancy, the present study measured the affinity of tramadol (and its enantiomers) and an active O-desmethyl metabolite (M1) (and its enantiomers) to cloned human opioid receptors of the μ, δ and κ type stably expressed in HN9.10 neuroblastoma cells. At μ sites, the Ki values for tramadol, its (+) and (−) enantiomers, M1, and its (+) and (−) enantiomers were 17 000, 15 700, 28 800, 3190, 153 and 9680 nM, respectively, compared to 7.1 nM for morphine. These results are consistent with the suggestion of a non-opioid contribution to the clinical profile of tramadol." @default.
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- W2065652085 date "1996-12-01" @default.
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- W2065652085 title "Tramadol, M1 metabolite and enantiomer affinities for cloned human opioid receptors expressed in transfected HN9.10 neuroblastoma cells" @default.
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- W2065652085 doi "https://doi.org/10.1016/s0014-2999(96)00770-4" @default.
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