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Distribution and excretion of a new insect repellent, 14C-DEM, in the mouse after intravenous, cutaneous, and oral administration.

The distribution of 14C after administration of 14C-DEM was qualitatively similar irrespective of the administration route (intravenous, cutaneous or oral). The major accumulation sites were lacrimal and nasal glands, parotis, liver, and kidney. The main excretion was through the urine and only minor quantities through the faeces and the expired gases. It could be confirmed that the new repellent had a low skin uptake.

Acetamides↗

Laboratory testing of the insect repellents IR3535 and DEET against Phlebotomus mascittii and P. duboscqi (Diptera: Psychodidae).

The efficacy of the repellent IR3535 was tested and compared with DEET using two laboratory colonies of phlebotomine sand flies, Phlebotomus mascittii and Phlebotomus duboscqi. P. duboscqi, originating from Senegal, is a proven vector of Leishmania major. P. mascittii (Corsican origin) has never been demonstrated to be a vector of leishmaniasis, but it was reported in 2004 as an anthropophilic species in Germany associated with autochthonous visceral leishmaniasis in people and animals. IR3535 and DEET were tested at an effective concentration of 10% in ethanol on two (one male, one female) human volunteers. The mean protection time against P. duboscqi was 5.9h for both repellents, against P. mascittii 10.4 and 8.8 h for IR3535 and DEET, respectively.

Animals↗

Stereochemical effects in an insect repellent.

Racemic 1-[3-cyclohexen-1-ylcarbonyl]-2-methylpiperidine repels blood-feeding arthropods such as mosquitoes, chiggers, and ticks. The compound contains two asymmetric carbon atoms and the racemate consists of four stereoisomers. Quantitative mosquito bioassays using Aedes aegypti (L.) showed that (1S,2'S) and (1R,2'S) configurations were 2.8-3.1 and 1.6-1.8 times more effective, respectively, than the other two stereoisomers in reducing mosquito bites. (1S,2'S) was 2.5 more repellent than the racemate. Biological data show that an interaction of the (2'S)-2-methylpiperidine configuration with a repellent receptor system in A. aegypti is apparently important to repellent activity. Nuclear magnetic resonance spectra and molecular mechanics calculations for the stereoisomers provided insight into the conformation of the (2'S)-group. Results indicate that enhanced repellent effects can be realized through formulation of the most active stereoisomers of the compound.

Aedes↗