A note on the effects of 2, 4-diainino-5-phenylthiazole and 1, 2, 3, 4-tetrahydro-9-aminoacridine on morphineChromatographs of extracts of urine from patients receiving mixtures of morphine plus amiphenazole or morphine plus 1,2,3,4-tetrahydro-9-aminoacridine (THA) have a spot which is due to a substance with properties similar to morphine-N-oxide. This spot was not present in urine of patients given morphine, amiphenazole or THA alone. Morphine-N-oxide may bc a metabolite o f morphine, and amiphenazole and THA may inhibit the further metabolism of morphine-N-oxide.HE use of combinations of 2,4-diamino-5-phenylthiazole (amiphena-Br. med. J., 2, 366-368.
After administration of morphine‐N‐oxide (MNO) to rats the opiates appearing in the urine were morphine (61%) and MNO (39%). After administration of morphine, the urinary opiates were morphine (80%) and normorphine (20%). When tacrine was given with morphine the urine also contained MNO (46% of total urinary opiates) and the amount of normorphine was much decreased (to 1%), the remainder being morphine (53%). Tacrine and amiphenazole inhibited demethylation of morphine and codeine by a rat liver fraction in vitro. MNO had weak inhibitory activity. Neither MNO nor codeine‐N‐oxide were demethylated in vitro.
1. The central depressant effects of bromvaletone, carbromal and six non-bromo analogues were compared in mice. 2. The chloro analogues of bromvaletone and carbromal were slightly less potent as central depressant agents than the bromo compounds. 3. The chloro analogue of bromvaletone had the greatest margin between central depressant and lethal doses. 4. Lipophilicity (octanol-water partition coefficient) did not provide a unifying relationship for potency within this group of eight acylureas. However, within each of the two subsets of compounds, a linear relationship was found between relative potency and lipophilicity.
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