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T8200

Sigma-Aldrich

Tofisopam

≥98% (HPLC), solid

Sinônimo(s):

7,8-Dimethoxy-1-(3,4-dimethoxyphenyl)-5-ethyl-4-methyl-5H-2,3-benzodiazepine, EGYT 341, Seriel

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About This Item

Fórmula empírica (Notação de Hill):
C22H26N2O4
Número CAS:
22345-47-7
Peso molecular:
382.45
Número CE:
244-922-3
Número MDL:
MFCD00823171
Código UNSPSC:
12352200
ID de substância PubChem:
24724636
NACRES:
NA.77

Ensaio

≥98% (HPLC)

forma

solid

controle de medicamentos

regulated under CDSA - not available from Sigma-Aldrich Canada

cor

white

solubilidade

DMSO: ~14 mg/mL
H2O: insoluble

cadeia de caracteres SMILES

CCC1C(C)=NN=C(c2ccc(OC)c(OC)c2)c3cc(OC)c(OC)cc13

InChI

1S/C22H26N2O4/c1-7-15-13(2)23-24-22(14-8-9-18(25-3)19(10-14)26-4)17-12-21(28-6)20(27-5)11-16(15)17/h8-12,15H,7H2,1-6H3

chave InChI

RUJBDQSFYCKFAA-UHFFFAOYSA-N

Aplicação

Tofisopam has been used for studying its biochemical mechanisms of actions using drug repositioning strategies.

Ações bioquímicas/fisiológicas

Studies have reported that tofisopam functions by blocking PDE4 (phosphodiesterase 4). Furthermore, the S-enantiomer of tofisopam is considered ten times more active than R-enantiomer.
Ligand for the GABAA receptor benzodiazepine modulatory site.

Nota de preparo

Tofisopam is soluble in DMSO at approximately 14 mg/ml. However, it is insoluble in water.

Pictogramas

Exclamation markEnvironment
GHS07,GHS09

Palavra indicadora

Warning

Frases de perigo

H302,H400

Declarações de precaução

P273 - P301 + P312 + P330

Classificações de perigo

Acute Tox. 4 Oral - Aquatic Acute 1

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 2

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Equipamento de proteção individual

dust mask type N95 (US), Eyeshields, Gloves

Certificados de análise (COA)

Busque Certificados de análise (COA) digitando o Número do Lote do produto. Os números de lote e remessa podem ser encontrados no rótulo de um produto após a palavra “Lot” ou “Batch”.

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Maria Tóth et al.
Journal of pharmaceutical and biomedical analysis, 41(4), 1354-1359 (2006-05-10)
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) bioanalytical method was developed and validated for the purpose of pharmacokinetic study of tofisopam. A
N P Vanchakova et al.
Bulletin of experimental biology and medicine, 148(2), 343-345 (2009-12-23)
The study demonstrated high anxiolytic activity of tenoten, which was not inferior to the anxiolytic effect of grandaxin. The positive changes persisted after termination of treatment in the tenoten group (but not in grandaxin group). Tenoten can be recommended for
Drug repositioning: identifying and developing new uses for existing drugs.
Ted T Ashburn et al.
Nature reviews. Drug discovery, 3(8), 673-683 (2004-08-03)
Michael D Cameron et al.
Drug metabolism and disposition: the biological fate of chemicals, 35(10), 1894-1902 (2007-07-25)
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 between the two enantiomers. The major metabolite in incubations of 500 ng/ml (approximately
N Bonnet et al.
Toxicology and applied pharmacology, 221(1), 111-118 (2007-03-27)
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 inhibitors (PDE, rolipram and tofisopam) on bone microarchitecture and biomechanical properties.
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