Three‐dimensional GABA receptor models successfully explained the structure–activity relationships of the bicyclophosphorothionates.ĬONCLUSION: The results indicate that minor structural modifications of blockers can change their selectivity for insect versus mammalian GABA receptors. Among the bicyclophosphorothionates synthesised to date, the former analogue exhibited the highest selectivity for housefly GABA receptors, with an IC 50 rat/IC 50 fly ratio of approximately 97. The 4‐isopentyl‐3‐isopropylbicyclophosphorothionate showed the highest affinity for housefly GABA receptors (IC 50 = 103 nM) among the analogues tested, while the 4‐cyclohexylbicyclophosphorothionate showed the highest affinity for rat GABA receptors (IC 50 = 125 nM). RESULTS: Introduction of an isopropyl group at the 3‐position enhanced the affinity of bicyclophosphorothionates for housefly GABA receptors and reduced the affinity towards rat GABA receptors. Twenty‐two bicyclophosphorothionates with different 3‐ and 4‐substituents were synthesised, and 4′‐ethynyl‐4‐ n‐propylbicycloorthobenzoate (EBOB) binding assays were performed to evaluate their affinities for housefly and rat GABA receptors.
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