6-MEMBERED CYCLIC PHOSPHONATE GABA ANTAGONISTS, 2,5-DISUBSTITUTED 1,3,2-DIOXAPHOSPHORINANES

Authors
OZOE Y MATSUMOTO K MOCHIDA K NAKAMURA T
Citation
Y. Ozoe et al., 6-MEMBERED CYCLIC PHOSPHONATE GABA ANTAGONISTS, 2,5-DISUBSTITUTED 1,3,2-DIOXAPHOSPHORINANES, Bioscience, biotechnology, and biochemistry, 59(12), 1995, pp. 2314-2316
Citations number
13
Categorie Soggetti
Biology,Agriculture,"Biothechnology & Applied Migrobiology","Food Science & Tenology
Journal title
Bioscience, biotechnology, and biochemistry → ACNP
ISSN journal
09168451
Volume
59
Issue
12
Year of publication
1995
Pages
2314 - 2316
Database
ISI
SICI code
0916-8451(1995)59:12<2314:6CPGA2>2.0.ZU;2-2
Abstract
The tuans isomer of yl)-5-tert-butyl-2-thiono-1,3,2-dioxaphosphorinane competitively inhibited the specific binding of S-35-tert-butylbicycl ophosphorothionate to rat brain membranes with an IC50 value of 0.52 m u M, and showed insecticidal activity against houseflies with an LD(50 ) value of 2.4 mu g/fly. This compound and its analogues acted as nonc ompetitive GABA(A) receptor antagonists (NGRAs), and phosphorus-contai ning cyclohexane skeletons may prove useful for the design of novel NG RAs.