3 years ago

Development of Tetramethylenedisulfotetramine (TETS) Hapten Library: Synthesis, Electrophysiological Studies, and Immune Response in Rabbits.

Development of Tetramethylenedisulfotetramine (TETS) Hapten Library: Synthesis, Electrophysiological Studies, and Immune Response in Rabbits.
Natalia Vasylieva, Tomas Cajka, Susan Hulsizer, Heike Wulff, Shirley J. Gee, Isaac Pessah, Hai M. Nguyen, Bruce D. Hammock, Bogdan Barnych, Tom Joseph
There is a need for fast detection methods for the banned rodenticide tetramethylenedisulfotetramine (TETS), a highly potent blocker of the γ-aminobutyric acid (GABAA) receptors. General synthetic approach toward two groups of analogues was developed. Screening of the resulting library of compounds by FLIPR or whole-cell voltage-clamp revealed that, despite the structural differences, some of the TETS analogues retained GABAA receptor inhibition; however, their potency was an order of magnitude lower. Antibodies raised in rabbits against some of the TETS analogues conjugated to protein recognized free TETS and will be used for the development of an immunoassay for TETS. Mimicking neurotoxic TETS: TETS and newly synthesized polycyclic sulfamides were shown to have similar GABAA receptor channel blocking properties and were both recognized by antibodies raised against synthetic TETS haptens.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/chem.201700783

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