About: Tracazolate is a research topic. Over the lifetime, 37 publications have been published within this topic receiving 2497 citations. The topic is also known as: ICI-136,753 & ICI-136753.
TL;DR: The current studies further investigated the effects, in animal models of anxiety, of novel putative anxiolytic and anxiogenic compounds believed to induce their effects by actions at the GABA-benzodiazepine receptor complex to provide further validation for a novel test of anxiety based on the ratio of open to closed arm entries in an elevated plus maze in the rat.
Abstract: The current studies further investigated the effects, in animal models of anxiety, of novel putative anxiolytic and anxiogenic compounds believed to induce their effects by actions at the GABA-benzodiazepine receptor complex. It was expected that the results would also provide further validation for a novel test of anxiety based on the ratio of open to closed arm entries in an elevated plus maze in the rat. The novel putative anxiolytics CL 218,872 (10–20 mg/kg) and tracazolate (5 mg/kg) significantly elevated the percentage of time spent on the open arms of an elevated plus-maze, consistent with their anxiolytic activity in several other animal tests. Also consistent with results from other animal tests, no anxiolytic activity was observed for the phenylquinoline PK 8165 (10–25 mg/kg), the 3,4-benzodiazepine tofisopam (25–50 mg/kg), or buspirone (0.5–20 mg/kg). The benzodiazepine receptor inverse agonists FG 7142 (1–5 mg/kg) and CGS 8216 (3–10 mg/kg) had anxiogenic activity in this test, as did the atypical benzodiazepine Ro 5-4864 (1–5 mg/kg). Interestingly, however, the benzodiazepine receptor antagonists Ro 15-1788 (10–20 mg/kg) and ZK 93426 (5–10 mg/kg) had no anxiogenic activity in this test.
TL;DR: Several new non-benzodiazepine anxiolytics are reported, including tracazolate, zopiclone, CL218,872, CGS9896, buspirone, MK-801 and fenobam, which enhance binding of [3H]-flunitrazepam in contrast to benzodiazepines which displace it.
TL;DR: All the anxiogenic drugs tested (CGS 8216, picrotoxin and yohimbine) produced conditioned aversion, suggesting that it is possible to dissociate the rewarding and anxiolytic properties of drugs.
TL;DR: Tracazolate (ICI 136,753) 4-butylamine-1-ethyl-6-methyl-1H-pyrazolo[3,4]pyridine-5-carboxylic acid ethyl ester is a non-benzodiazepine with anxiolytic-like activity in animal models and enhances [3H]flunitrazepam binding in rat synaptic membrane fragments.
TL;DR: It is apparent that the anticonflict activity of agents that bind to benzodiazepine receptors is blocked by benzodiazine antagonists, and the activity of anxiolytics that are not displacers are unaffected even at higher doses.