EFFECTS OF SELECTED IMIDAZOPYRIMIDINE LIGANDS FOR BENZODIAZEPINE RECEPTORS IN RODENT MODELS OF ANXIETY AND BEHAVIORAL IMPAIRMENT

A group of imidazopyrimidine ligands of benzodiazepine receptors has been shown to produce anti-conflict effects in a punished rat operant task, at comparable doses to classical benzodiazepine agonists such as diazepam. Most were able to attenuate the convulsant effects of pentylenetetrazole and electroshock in the mouse, although with reduced potency compared with the reference classical benzodiazepines. Their activity in tests of functional central nervous system impairment (rotating drum and potentiation of phenobarbitone in the mouse, potentiation of chloral hydrate and pull-up test in the rat) was also markedly less than the classical agonists. These data are consistent with these imidazopyrimidines being partial agonists at the benzodiazepine receptor.