2. Academic Validation
  3. 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

  • Chemistry. 2017 Jun 22;23(35):8466-8472. doi: 10.1002/chem.201700783.
Bogdan Barnych 1,  Natalia Vasylieva 1,  Tom Joseph 1,  Susan Hulsizer 2,  Hai M Nguyen 3,  Tomas Cajka 4,  Isaac Pessah 2,  Heike Wulff 3,  Shirley J Gee 1,  Bruce D Hammock 1
Affiliations

Affiliations

  • 1 Department of Entomology and Nematology, and UCD Comprehensive Cancer Center, University of California Davis, Davis, California, 95616, United States.
  • 2 Department of Molecular Biosciences, School of Veterinary Medicine, University of California Davis, Davis, California, 95616, United States.
  • 3 Department of Pharmacology, School of Medicine, University of California Davis, Davis, California, 95616, United States.
  • 4 UC Davis Genome Center-Metabolomics, University of California Davis, Davis, California, 95616, United States.
PMID: 28411375 DOI: 10.1002/chem.201700783
Abstract

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.

Keywords

GABA; antibodies; cage convulsants; neurotoxicity; poly-heterocycles; tetramine.

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