- Guide to PHARMACOLOGY
Compound class: Natural product or derivative
Comment: Tetrodotoxin is a potent neurotoxin found in certain fish and other aquatic animals, although it is actually produced in symbiotic bacteria hosted in these creatures.
There is some ambiguity in the literature and on other databases as to the exact stereochemistry of tetrodotoxin. Our structure matches that on ChEBI and the PubChem entry linked to above, while the compound is also represented by the alternative isomer in CHEMBL507974 and CID 11174599.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: tetrodotoxin
|No information available.|
|Summary of Clinical Use|
|Subcutaneous tetrodotoxin has been evaluated in a Phase 3 clinical trial for its capacity to alleviate moderate to severe inadequately controlled cancer-related pain (NCT00725114).|
|Mechanism Of Action and Pharmacodynamic Effects|
|Mechanistically, tetrodotoxin blocks voltage-gated sodium channels to prevent the rising phase of the action potential. Tetrodotoxin poisoning causes loss of sensation, paralysis of voluntary muscles including the diaphragm and intercostal muscles which compromises respiration. Tetrodotoxin poisoning is serious but not always fatal.|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT00725114||Safety & Efficacy Study of Subcutaneous Tetrodotoxin for Moderate to Severe Inadequately Controlled Cancer-related Pain||Phase 3 Interventional||Wex Pharmaceuticals Inc.|