CL 218,872

CL 218,872 is an anxiolytic agent.¹ It selectively binds to α₁β₁γ₂ subunit-containing GABA_A receptors over α₂β₁γ₂ or α₃β₁γ₂ subunit-containing GABA_A receptors (K_is = 0.131, 1.82, and 1.53 µM, respectively).² CL 218,872 increases drinking in the Vogel punished drinking task and inhibits foot-shock-induced fighting, indicating anxiolytic-like activities, in mice in a dose-dependent manner.¹ It also increases the duration of pentobarbitone-induced anesthesia, reduces spontaneous locomotor activity, and inhibits convulsions induced by pentylenetetrazole (PTZ; Item No. 18682), picrotoxin (Item No. 20771), or bicuculline (Item No. 11727) with ED₅₀ values of 12.8, 28.5, and 35.3 mg/kg, respectively, in mice.¹

WARNING This product is not for human or veterinary use.

1. Oakley, N.R., Jones, B.J., and Straughan, D.W. The benzodiazepine receptor ligand CL218,872 has both anxiolytic and sedative properties in rodents. Neuropharmacology 23(7A), 797-802 (1984).

2. Pritchett, D.B., Lüddens, H., and Seeburg, P.H. Type I and type II GABA_A-benzodiazepine receptors produced in transfected cells. Science 245(4924), 1389-1392 (1989).