Metabolism of profluralin in rats. 1. Identification of metabolites

Abstract

Fluorine NMR spectroscopy has been used to identify and quantitate metabolites of profluralin appearing in the urine of rats postingestion of the herbicide. The chemical shift of the trifluoromethyl group was shown to be a useful indicator of the chemical type of metabolite, and the shifts for the classes of materials previously identified as metabolites have been determined. By use of chemical shift criteria this work provides evidence for several metabolites that have not been recognized in previous work; some of these remain incompletely characterized. Though the number and types of metabolites detected in the urine were consistent from animal to animal, the time course for appearance of metabolites was found to be animal dependent.

Camel (Camelus spp.) Urine Bioactivity and Metabolome: A Systematic Review of Knowledge Gaps, Advances, and Directions for Future Research

“…On the other hand, the fact that certain chemicals could only be exclusively found in one study may reflect the potential variability in urine composition and bioactive effects across different camel subjects, breeds, and populations for animal-related factors influencing metabolism such as sex [ 100 , 101 ], age [ 102 ], diet [ 97 , 103 ], environmental seasonality [ 104 , 105 ], composition of gut microbiome [ 106 , 107 ], and the kinetics of the reactions leading to the production of metabolites or the time course of metabolism [ 108 ]. For these reasons, it is strongly recommended that details on the animals’ sex, age, physiological status, rearing conditions (desert-living vs. farming), and diet formulation/composition are provided alongside the animal subjects or groups from which the urine was collected.…”

Synthesis, Structural Determination, and Pharmacology of Putative Dinitroaniline Antimalarials

“…1 is rapidly cleared in rats by faecal and urinary excretion with only 10 % remaining unmetabolised . Rapid metabolism and clearance in rodents may account for the inactivity of 1 in rodent models of Plasmodium and Cryptosporidium in vivo . Another possibility is that the high log P value of 1 (4.81) constrains this substance at or around the site of injection …”

“…[35] 1 is rapidly cleared in rats by faecal and urinary excretion with only 10 % remaining unmetabolised. [36] Rapid metabolism and clearance in rodents [37] may account for the inactivity of 1 in rodent models of Plasmodium and Cryptosporidium in vivo. Another possibility is 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 that the high log P value of 1 (4.81) constrains this substance at or around the site of injection.…”