Six-membered cyclic phosphonate GABA antagonists, 2,5-disubstituted 1,3,2-dioxaphosphorinanes.

Article abstract of DOI:10.1271/bbb.59.2314

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.

Full text of DOI:10.1271/bbb.59.2314

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Six-membered Cyclic Phosphonate GABA Antagonists,
2
, 5-Disubstituted 1,3,2-Dioxaphosphorinanes
a a a a
Yoshihisa Ozoe , Ken-ichi Matsumoto , Kazlio Mochida & Toshiie Nakamura
a
Department of Bioresource Science, Faculty of Agriculture, Shimane University,
Matsue, Shimane 690, Japan
Published online: 12 Jun 2014.
To cite this article: Yoshihisa Ozoe, Ken-ichi Matsumoto, Kazlio Mochida & Toshiie Nakamura (1995) Six-membered
Cyclic Phosphonate GABA Antagonists, 2, 5-Disubstituted 1,3,2-Dioxaphosphorinanes, Bioscience, Biotechnology, and
Biochemistry, 59:12, 2314-2316, DOI: 10.1271/bbb.59.2314
To link to this article: http://dx.doi.org/10.1271/bbb.59.2314
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