Mebicar
(Synonyms: 2,4,6,8-四氮杂双环[3.3.0]辛烷-3,7-二酮,2,4,6,8-四甲基-,Tetramethylglycoluril; Mebicar) 目录号 : GC49319An anxiolytic with antiepileptic activity
Cas No.:10095-06-4
Sample solution is provided at 25 µL, 10mM.
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Mebicar is an anxiolytic with antiepileptic activity.1,2 In vivo, mebicar (10 mg/kg) reduces anxiety-like behavior and decreases stress-induced increases in serum corticosterone and pro-inflammatory cytokine levels in a mouse model of intermittent unpredictable stress.1 It inhibits epileptic activity in a rat model of penicillin-induced focal epilepsy.2
1.Kim, C.Y., Kim, Y.G., Sin, S.J., et al.Preventive effect of mebicar and ginsenoside Rg1 on neurobehavioral and immunological disruptions caused by intermittent unpredictable stress in miceNeuroImmunoModulation25(1)49-58(2018) 2.Rekhtman, M.B., Torshin, V.I., and Darinski?, N.V.Effect of mebikar on focal epileptic activityBiull. Eksp. Biol. Med.91(2)178-181(1981)
Cas No. | 10095-06-4 | SDF | |
别名 | 2,4,6,8-四氮杂双环[3.3.0]辛烷-3,7-二酮,2,4,6,8-四甲基-,Tetramethylglycoluril; Mebicar | ||
Canonical SMILES | O=C1N(C2N(C)C(N(C2N1C)C)=O)C | ||
分子式 | C8H14N4O2 | 分子量 | 198.2 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 25 mg/ml,PBS (pH 7.2): 10 mg/ml | 储存条件 | -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 5.0454 mL | 25.227 mL | 50.4541 mL |
5 mM | 1.0091 mL | 5.0454 mL | 10.0908 mL |
10 mM | 0.5045 mL | 2.5227 mL | 5.0454 mL |
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Preventive Effect of Mebicar and Ginsenoside Rg1 on Neurobehavioral and Immunological Disruptions Caused by Intermittent Unpredictable Stress in Mice
Neuroimmunomodulation 2018;25(1):49-58.PMID:29920498DOI:10.1159/000489634.
Objectives: Ginsenoside Rg1 and Mebicar have been reported to have broad efficacy spectrum, including anti-anxiety and anti-stress. These drugs have been used not only for treatment but also for the purpose of increasing resistance from disease. A specific aim of this study was to investigate whether Mebicar or ginsenoside Rg1 can prevent physiological changes resulting from intermittent unpredictable stress (IUS). Methods: Seven week-old Balb/cByJ mice were administered orally with Mebicar (10 mg/kg) or ginsenoside Rg1 (10 mg/kg) starting from a week before they were exposed to IUS until the end of the experiment. IUS, which consists of psychological stress and physical fatigue, was set as 3 bouts (24 h/bout) exposure in a 2-week period. Results: IUS caused hyperactivity and anxiety-like behavior, which were not inhibited by Mebicar or ginsenoside Rg1. IUS mice treated with Mebicar or ginsenoside Rg1 recovered rapidly from anxiety-like behavior induced by the multiplexed stress compared to the mice not orally treated with Mebicar or ginsenoside Rg1. Mebicar or ginsenoside Rg1 could not prevent the decrease of brain-derived neurotropic factor by IUS exposure. However, Mebicar or ginsenoside Rg1 prevented elevation of serum corticosterone and secretion of proinflammatory cytokines from splenocytes due to IUS exposure. Conclusions: This study suggests that Mebicar or ginsenoside Rg1 may have little preventive effect on neurobehavioral disruption by IUS exposure, but Mebicar or ginsenoside Rg1 shortened the lasting duration of the anxiety caused by exposure to a novel environment. The anti-stress effect of Mebicar and ginsenoside Rg1 may be restricted in peripheral stress responses.
[An experience of using Mebicar in patients with autonomic dysfunction associated with anxiety disorder]
Zh Nevrol Psikhiatr Im S S Korsakova 2017;117(11):56-63.PMID:29265088DOI:10.17116/jnevro201711711156-63.
Background: Cognitive impairments are one of the most frequent and maladaptive factors in patients with autonomic dysfunction associated with anxiety disorder. The majority of anxiolytics manage to compensate anxiety but suppress cognitive functions. Material and methods: Fifty-four patients with autonomic dysfunction and anxiety disorder, including 39 women (mean age 25±6.7 years) and 15 men (mean age 27±8.4 years), were treated with Mebicar during 3 months. Results and conclusion: A reduction in the degree of autonomic dysfunction and anxiety symptoms as well as a significant improvement of cognitive functions were noted. Mebicar showed a good tolerability and minimum drug-related adverse events, and can be recommended as a first line anti-anxiety remedy in wide clinical practice.
[Experimental comparative study of the analgesic activity of the diurnal anxiolytic Mebicar, amitriptyline, and diazepam]
Eksp Klin Farmakol 2015;78(3):9-12.PMID:26036004doi
It is established that Mebicar, amitriptyline, and diazepam administered intraperitoneally at therapeutic doses increase the pain thresholds in mice as manifested in "hot plate" analgesia test. Mebicar was more effective than diazepam and not inferior to amitriptyline in increasing the pain thresholds at earlier time points.
[Anti-inflammatory effects of amitriptyline, diazepam and Mebicar using model of acute carrageenan-induced paw edema in rats]
Eksp Klin Farmakol 2011;74(12):19-22.PMID:22379877doi
The anti-inflammatory activity of amitriptyline, diazepam and a new, Russian tranquilizer Mebicar was studied in a wide range of therapeutic doses on carrageenan-induced paw edema in rats. Mebicar at low doses showed greater and longer (up to 24 h) lasting anti-inflammatory activity as compared to that of amitriptyline and diazepam.
[Characteristics of the psychotropic spectrum of action of Mebicar]
Biull Eksp Biol Med 1980 May;89(5):568-70.PMID:6104993doi
Under group interaction in cats, a new Soviet tranquilizer Mebicar eliminates fear-alarm induced by stimulatin of the emotiogenic zone of the hypothalamus. This action is not associated with myorelaxant or hypnotic action. Mebicar decreases the brain noradrenaline level, exerts no effect on the dopaminergic systems, increases the brain serotonin level, and does not elicit cholinolytic action.