Pharmacokinetics, metabolism and toxicity of the plant-derived photoxin alpha-terthienyl.

R Marles, T Durst, M Kobaisy, C Soucy-Breau, M Abou-Zaid, J T Arnason, S Kacew, D Kanjanapothi, C Rujjanawate, M Meckes

Ottawa-Carleton Institute of Chemistry, University of Ottawa, Ont., Canada.

Pharmacology & toxicology 1995 Sep

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The plant-derived insecticide, alpha-terthienyl was prepared by synthesis as 3',4'-di[14C]-alpha-terthienyl for pharmacokinetic and metabolism studies. When administered orally to rats at a single dose of 50 mg/kg, excretion of the labelled material was maximal one day after administration and declined to no measurable quantities by day 4. Two metabolites [1,4-di(2'-thienyl)1,4-butadione and 2-2'-bithiophene-5-carboxylic acid] and trace quantities of the parent material were isolated from the urine and chemically identified. These represent the first metabolites of alpha-terthienyl identified. In pilot acute and subacute trials, unlabelled alpha-terthienyl was non-toxic when administered orally to rats as the "ready to use" formulation (0.1% active ingredient). The pure compound had an LD50 of 110 mg/kg when administered intraperitoneally to rats. The results suggest that there is considerable separation with respect to mosquito larvae and non-target mammal sensitivity.

Citation

R Marles, T Durst, M Kobaisy, C Soucy-Breau, M Abou-Zaid, J T Arnason, S Kacew, D Kanjanapothi, C Rujjanawate, M Meckes. Pharmacokinetics, metabolism and toxicity of the plant-derived photoxin alpha-terthienyl. Pharmacology & toxicology. 1995 Sep;77(3):164-8