a neuronal voltage-dependent and GABA-gated Cl- channels blocker; non-competitive GABA antagonist; causes epileptoform seizures.

Organophosphorous compound C₆H₁₁O₄P, synthetic.

• Molecular Weight : 178 Da.
  
  
• Melting Point : 201-202 °C.
  
  
• Solubility in : well in alcohol and water.
  
  
• Purity min. : 95 % (NMR).
  
  
• Biological Activity : Cl- channel total blocking concentration: IC₁₀₀ ~ 50 nM (Lymnaea stagnalis); (IC50) for [3H]-dihydropicrotoxin binding with rat brain membrane P2 fraction: 5.0 µM (Ticku M.);
  (IC50) for [35S]-tert.butyl-thionebicyclophosphate binding with human brain membranes : 5.9 µM (Casida J.);
  experiments with [3H]-labelled GABA-competitive ligands (Muscimol, Funitrazepam) showed no influence of Etbicyphat up to 10 µM.
  
  
• Toxicity (LD₅₀) : mice (i.p.): 1.0 mg/kg.
  mice (i.v.): 0.35 mg/kg.
  
  
• Storage recommendations : store at room temperature.
  
  
• CAS Reg. No. : 1005-93-2
  
  
• Bibliography :
  
  1. Bellet et al., Science.(1973) 182:1135-1136
  2. Cooper G. H. et al., Eur. J. Med. Chem. (1978). 13:207-212
  3. Fetisov et al., Biol. Membr. (1986) (Russian). 3(5):968-970
  4. Squires et al., Mol. Pharmacol.(1983) 23:326-331