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Updated: Aug 19, 2026

Preparation and Reactivity of a Triphosphenium Bromide Salt: A Convenient and Stable Source of Phosphorus(I)
Published on: November 22, 2016
Six-membered cyclic phosphonate GABA antagonists, 2,5-disubstituted 1,3,2-dioxaphosphorinanes
Y Ozoe1, K Matsumoto, K Mochida
1Department of Bioresource Science, Faculty of Agriculture, Shimane University, Japan.
Abstract:
The trans isomer of 2-(4-bromophenyl)-5-tert-butyl-2-thiono-1,3,2-dioxaphosphorinane competitively inhibited the specific binding of 35S-tert-butylbicyclophosphorothionate to rat brain membranes with an IC50 value of 0.52 microM, and showed insecticidal activity against houseflies with an LD50 value of 2.4 micrograms/fly. This compound and its analogues acted as noncompetitive GABAA receptor antagonists (NGRAs), and phosphorus-containing cyclohexane skeletons may prove useful for the design of novel NGRAs.
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