a non-competitive GABA antagonist; potent convulsant: causes epileptoform seizures.

Organophosphorous compound, C₇H₁₃O₄P, synthetic.

• Molecular Weight : 192 Da.
  
  
• Melting Point : 222-223 °C
  
  
• Solubility in : well in alcohol and water.
  
  
• Purity min. : 95 % (NMR).
  
  
• Biological Activity : (IC50) for blocking the GABA-dependent [36Cl] uptake in rat brain synaptosomes: 0.2 nM.
  (IC50) for the inhibition of [3H]-dihydropicrotoxin binding with the rat brain membrane P2 fraction: 8.0 µM; (Ticku M.);
  (IC50) for the inhibition of [35S]-tert.butyl-thionebicyclophosphate binding with human brain membranes: 480 nM. (Casida J.E.);
  experiments with [3H]-labeled GABA-competitive ligands (muscimol, flunitrazepam) showed no influence of Isobicyphat up to 10 µM.
  
  
• Toxicity (LD₅₀) : mice (i.p.): 0.18 mg/kg.
  mice (i.v.): 0.31 mg/kg.
  
  
• Storage recommendations : store at room temperature.
  
  
• CAS Reg. No. : 51052-72-3
  
  
• Bibliography :
  
  1. Bellet E. M., Casida J. E., Sciences (1973). 182:1135-1136
  2. Cooper et al., Mol. Pharmacol. (1983). 23:207-212
  3. V. I. Fetisov et al., Biol. Membr.(1986) (Russian). 3(5):968-970
  4. Squires et al., Mol. Pharmacol.(1983) 23:326-331