a GABA-gated chloride channel blocker, non-competitive GABA antagonist in mammals.

Organophosphorous compound, C₇H₁₃O₄P, synthetic.

• Molecular Weight : 192 Da.
  
  
• Melting Point : 234-236 °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: 0.5 nM;
  inhibition of the GABA-dependent Cl- current at 1.09 nM;
  (IC50) for [3H]-dihydropicrotoxin binding with the rat brain membrane P2 fraction: 8.0 µM (Ticku M.);
  (IC50) for [35S]-tert.butyl-thionebicyclophosphate binding with the human brain membranes: 1.1 µM (Casida J.);
  experiments with [3H]-labelled GABA-competitive ligands (Muscimol, Flunitrazepam) showed no influence of Propybicyphat up to 10 µM.
  
  
• Toxicity (LD₅₀) : mice (i.p.): 0.38 mg/kg.
  
  
• Storage recommendations : store at room temperature
  
  
• CAS Reg. No. : 51486-74-9
  
  
• Bibliography :
  
  1. Bellet et al., Science.(1973) 182:1135-1136
  2. Squires et al., Mol. Pharmacol.(1983) 23:326-336
  3. Fetisov et al., Biol. Membr. (1986) (Russian). 3(5):968-970
  4. Cooper et al., Mol. Pharmacol. (1983). 23:207-212