Synthesis and Testing of Tetrodotoxin and Batrachotoxin Antagonists

摘要

Compounds have been synthesized as potential antagonists to the neurotoxinbatrachotoxin. The compounds synthesized have been examined for binding affinity at the batrachotoxin binding site in rat brain, and for ability to inhibit veratridine-stimulated (22)Na+ uptake into neuroblastoma cells. The compounds ranged in affinity from 2.7 to 200 micrometers. The compounds also varied in their abilities to stimulate or inhibit (22)Na+. The two highest affinity