2017
DOI: 10.1134/s1819712417040043
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An effector analysis of the interaction of propoxazepam with antagonists of GABA and glycine receptors

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Cited by 16 publications
(19 citation statements)
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“…In our studies, the «dose-effect» curve of the protective effect of propoxazepam on the 4-AP-induced model of convulsion has a S-shaped shape, but even at high propoxazepam doses (80 mg/kg) 100% effect is not reached. This is similar to propoxazepam anticonvulsive action in the strychnine-induced seizures model [4] and may also indicate that the anticonvulsant effect of the test compound is not receptor-agonistic, but through the different mediatory systems, the effectiveness of the interaction between which determines the maximal effect achieved. However, the slope of the curve (s) is 1.15, which corresponds to the receptor mechanism of interaction with the effect increasing within wide doses range (approximately 1.0 per log scale).…”
Section: R E S U L T S a N D Discussionsupporting
confidence: 56%
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“…In our studies, the «dose-effect» curve of the protective effect of propoxazepam on the 4-AP-induced model of convulsion has a S-shaped shape, but even at high propoxazepam doses (80 mg/kg) 100% effect is not reached. This is similar to propoxazepam anticonvulsive action in the strychnine-induced seizures model [4] and may also indicate that the anticonvulsant effect of the test compound is not receptor-agonistic, but through the different mediatory systems, the effectiveness of the interaction between which determines the maximal effect achieved. However, the slope of the curve (s) is 1.15, which corresponds to the receptor mechanism of interaction with the effect increasing within wide doses range (approximately 1.0 per log scale).…”
Section: R E S U L T S a N D Discussionsupporting
confidence: 56%
“…The propoxazepam average effective dose for this test was 37.3 ± 7.9 mg/kg, which is almost twice that of strychnine (16.4 ± 6.1 mg/kg) and also indicates that it has no significant effect directly to this type of receptor. For a real antagonist of GABA-R picrotoxin, this value is 1.67 ± 0.09 mg/kg [4]. Based on the anticonvulsive effect value in this test, it can be concluded that propoxazepam does not exhibit direct and pronounced action on potassium channels that are blocked by the 4-AP.…”
Section: R E S U L T S a N D Discussionmentioning
confidence: 77%
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“…The anticonvulsant effect of propoxazepam was evaluated on mice as the relative number of surviving animals that were recorded 2 hours after the convulsant administration. The tested compound was administered intraperitoneally (in a Tween-80 emulsion) [8,9]. Chemoconvulsant solution (picrotoxin 6.5 mg/kg) is dose that causes lethal effects in 95% of tested animals was administered subcutaneously to animals (6-8 animals in each experimental group) 30 min after propoxazepam administration.…”
Section: Anticonvulsant and Antinociceptive Activity Test -Tail-flickmentioning
confidence: 99%
“…One of them, Propoxazepam, 7-bromo-5-(o-chlorophenyl)-3-propoxy-1,2-dihydro-3H-1,4-benzodiazepin-2-one, is considered a promising drug and is undergoing preclinical trials [6]. Similar to gabapentin and pregabalin, which are well-known drugs used in general medical practice in the treatment of neuropathic pain [7], propoxazepam also has an anticonvulsant effect [8,9], which explains the analgesic component of the pharmacological spectrum…”
Section: Introductionmentioning
confidence: 99%