Synthesis and testing of tetrodotoxin and batrachotoxin antagonists. Final report, 1 February 1986-15 September 1989
Technical Report
·
OSTI ID:7226945
Compounds have been synthesized as potential antagonists to the neurotoxin batrachotoxin. 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 compounds proved to be complete antagonists, competitively inhibiting both basal- and veratridine-stimulated (22)Na+ uptake. Neither of these compounds protected against batrachotoxin-induced lethality in mice. We have also made some progress in the synthesis of potential antagonists to the neurotoxin tetrodotoxin.
- Research Organization:
- SRI International, Menlo Park, CA (United States)
- OSTI ID:
- 7226945
- Report Number(s):
- AD-B-143492/7/XAB; CNN: DAMD17-86-C-6060
- Country of Publication:
- United States
- Language:
- English
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