[Assessment of anxiolytics (3)--biochemical approach].
Synaptoneurosomes are entities in which a presynaptic sac (synaptosome) is attached to a resealed postsynaptic vesicle (neurosome). Biochemical studies have demonstrated that the synaptoneurosomes retain several receptor-mediated activities such as accumulations of cyclic AMP and ion fluxes. GABAA receptor-mediated 36Cl- uptake and modulatory effects of the uptake by benzodiazepines, barbiturates and neurosteroids have been reported in rat brain synaptoneurosomes. The in vitro protocol of the GABAA receptor ligand-stimulated 36Cl- influx proves to be of value for the screening of new compounds such as anxiolytics.
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Department of Pharmacology, College of Pharmacy, Nihon University, Funabashi, Japan.
D000818:Animals; D014151:Anti-Anxiety Agents; D001569:Benzodiazepines / Q000494:pharmacology; D002713:Chlorine / Q000493:pharmacokinetics; D000242:Cyclic AMP / Q000378:metabolism; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D011963:Receptors, GABA-A / Q000378:metabolism; D013574:Synaptosomes / Q000502:physiology
D014151:Anti-Anxiety Agents; D011963:Receptors, GABA-A; D001569:Benzodiazepines; D002713:Chlorine; D000242:Cyclic AMP