Opioid Pharmaceutical Intermediates U 48800 research chemical Powders CAS 82657-23-6
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Systematic (IUPAC) name: 3,4-Dichloro-N-[(1R,2R)-2-(dimethylamino)cyclohexyl]-N-methylbenzamide
U-48800 is an opioid analgesic drug developed by a team at Upjohn in the 1970s that acts as a selective agonist of the µ-opioid receptor with a Kd value of 5.3 nM compared to 910 nM for the κ-opioid receptor and has around 7.5 x the potency of morphine in animal models.
U-48800 is a structural isomer of the earlier opioid AH-7921 and the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold. Upjohn looked for the key moieties which gave the greatest activity and posted over a dozen patents on related compounds, each optimizing one moiety until they discovered that U-48800 was the most active.
U-48800 became the lead compound of selective kappa-opioid receptor ligands such as U-50488, U-51754 (containing a single methylene spacer difference) and U-69,593, which share very similar structures.
Although not used medically, the selective kappa ligands are used in research.
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