Tofisopam
Tofisopam structure
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Common Name | Tofisopam | ||
|---|---|---|---|---|
| CAS Number | 22345-47-7 | Molecular Weight | 565.593 | |
| Density | 1.2±0.1 g/cm3 | Boiling Point | 479.0±45.0 °C at 760 mmHg | |
| Molecular Formula | C18H39N5O13S | Melting Point | 155-159ºC | |
| MSDS | USA | Flash Point | 195.2±21.2 °C | |
| Symbol |
GHS07, GHS09 |
Signal Word | Warning | |
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The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis.
J. Neural Transm. Gen. Sect. 117(11) , 1319-25, (2010) Tofisopam is a member of the 2,3-benzodiazepine compound family which is marketed for the treatment of anxiety in some European countries. In contrast to classical 1,4-benzodiazepines, the compound does not bind to the benzodiazepine binding site of the γ-ami... |
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[Pineal hormone melatonin in low doses potentiates psychotropic and chronotropic activity of tofisopam in rats].
Eksp. Klin. Farmakol. 76(4) , 15-7, (2013) Combination with a low dose of pineal hormone melatonin increased the anxiolytic effect of tofisopam (subthreshold dose) in open-field and cross-maze tests, as well as its chronotropic activity in time-course of forced swimming test in rats. |
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Clinical trial: dextofisopam in the treatment of patients with diarrhoea-predominant or alternating irritable bowel syndrome.
Aliment. Pharmacol. Ther. 27(2) , 197-206, (2008) Dextofisopam modulates stimulated activity in animal models of stress, altered bowel motility, and visceral hypersensitivity.To evaluate the effects of dextofisopam in men and women with diarrhoea-predominant or alternating irritable bowel syndrome (IBS) (d-I... |
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Various effects of antidepressant drugs on bone microarchitectecture, mechanical properties and bone remodeling.
Toxicol. Appl. Pharmacol. 221(1) , 111-8, (2007) The aim of this study was to evaluate the effects of various drugs which present antidepressant properties: selective serotonin-reuptake inhibitors (SSRIs, fluoxetine), serotonin and noradrenaline-reuptake inhibitors (Desipramine) and phosphodiesterase inhibi... |
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Method validation and determination of enantiomers and conformers in tofisopam drug substances and drug products by chiral high-performance liquid chromatography and kinetic and thermodynamic study of the interconversion of the conformers.
J. Chromatogr. A. 1129(1) , 47-53, (2006) 1-(3,4-Dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine (tofisopam) contains one chiral center, so two enantiomeric forms exist. The ring system of tofisopam possesses two sterically stable boat structures, leading to two distinct conform... |
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In vitro prediction and in vivo verification of enantioselective human tofisopam metabolite profiles.
Drug Metab. Dispos. 35(10) , 1894-902, (2007) In vitro studies were conducted to elucidate the metabolic profiles of and the enzymes responsible for the metabolism of (R)- and (S)-tofisopam (1-(3,4-dimethoxyphenyl)-5-ethyl-7,8-dimethoxy-4-methyl-5H-2,3-benzodiazepine). Large differences were observed bet... |
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Gas chromatography nitrogen phosphorous detection (GC-NPD) assay of tofisopam in human plasma for pharmacokinetic evaluation.
J. Pharm. Biomed. Anal. 41(4) , 1354-9, (2006) Tofisopam (1-(3,4-dimethoxyphenyl)-4-methyl-5-ethyl-7,8-dimethoxy-5H-2,3-benzodiazepine) has been shown to be an effective anxiolytic agent in the wide-ranging clinical practice. A high sensitive gas chromatography nitrogen phosphorous detection (GC-NPD) bioa... |
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Tofisopam inhibits the pharmacokinetics of CYP3A4 substrate midazolam.
Eur. J. Clin. Pharmacol. 64(1) , 93-4, (2008)
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Analysis of tofisopam in human serum by column-switching semi-micro high-performance liquid chromatography and evaluation of tofisopam bioequivalency.
Biomed. Chromatogr. 16(4) , 277-81, (2002) A rapid and sensitive column-switching semi-micro HPLC method is described for the direct analysis of tofisopam in human serum. The sample (100 microL) was directly injected onto the precolumn (Capcell Pak MF Ph-1), where unretained proteins were eluted to wa... |
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[A case in which tofisopam was effective for treatment of paroxysmal supraventricular tachycardia].
Yakugaku Zasshi 123(5) , 365-8, (2003) Paroxysmal supraventricular tachycardia (PSVT) is a reentrant tachycardia, and the autonomic nervous system influences the paroxysms of PSVT. Tofisopam (Grandaxin) is a derivative of benzodiazepines. It is reported that heart rate variability (HRV) reveals th... |