论文信息 - Evidence for the pharmacological relevance of benzodiazepine receptors to anticonvulsant activity.

Evidence for the pharmacological relevance of benzodiazepine receptors to anticonvulsant activity.

Each of a series of benzodiazepines was found to be effective in preventing convulsions evoked by intermittent photic stimulation of epileptic chickens. There was a high correlation between the anticonvulsant potencies (mean effective dosages) and the affinity of the agents for the putative benzodiazepine receptor as measured by displacement of [3H]diazepam from binding sites on chicken synaptosomal membranes. This correlation in a genetic model of epilepsy provides further evidence that benzodiazepines exert their anticonvulsant effects by interacting with the benzodiazepine receptor.

T. Fisher | J. Tuchek | D. Johnson | R. D. Crawford

[1] D. Nutt,et al. On the convulsant action of Ro 5-4864 and the existence of a micromolar benzodiazepine binding site in rat brain , 2004, Psychopharmacology.

[2] C. Braestrup,et al. Audiogenic seizures in DBA/2 mice discriminate sensitively between low efficacy benzodiazepine receptor agonists and inverse agonists. , 1983, Life sciences.

[3] H. Mohler,et al. Benzodiazepine receptor: demonstration in the central nervous system , 1977, Science.

[4] C. Braestrup,et al. Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding. , 1977, Proceedings of the National Academy of Sciences of the United States of America.

[5] C. Coutinho,et al. The role of substituents in the hydrophobic binding of the 1,4-benzodiazepines by human plasma proteins. , 1976, Molecular pharmacology.

[6] A. Matus,et al. Isolation of synaptic plasma membrane from brain by combined flotation-sedimentation density gradient centrifugation. , 1974, Biochimica et biophysica acta.

[7] E. C. Crichlow,et al. Epileptiform seizures in domestic fowl. II. Intermittent light stimulation and the electroencephalogram. , 1974, Canadian journal of physiology and pharmacology.

[8] L. Stark,et al. The anticonvulsant effects of phenobarbital, diphenylhydantoin and two benzodiazepines in the baboon, Papio papio. , 1970, The Journal of pharmacology and experimental therapeutics.