Afobazole - CAS 173352-21-1
Catalog number: 173352-21-1
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C15H21N3O2S
Molecular Weight:
307.41
COA:
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Targets:
Others
Description:
Fabomotizole (brand name Afobazole) is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Its mechanism of action remains poorly defined however, with GABAergic, NGF- and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors. Clinical trials have shown fabomotizole to be well tolerated and reasonably effective for the treatment of anxiety. Experiments of mice have showed antimutagenic and antiteratogenic properties.
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Purity:
>98%
Synonyms:
CM346; Afobazol; Fabomotizole; CM 346; CM-346
MSDS:
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1.[THE STUDY OF ANXIOLYTIC PROPERTIES OF NEW PYRAZOLO[C]PYRIDINE DERIVATIVE GIZH-72].
Kudryashov NV, Kalinina TS, Shimshirt AA, Korolev AO, Volkova AV, Zhmurenko LA, Voroninal TA. Eksp Klin Farmakol. 2015;78(11):3-7.
It was studied the anxiolytic properties of 4,6-dimethyl-2-(4-chlorophenyl)-2,3-dihydro-1Í-pyrazolo[4,3-c]pyridin-3-one chloralhydrate (GIZh-72, 20 mg/kg, i.p.) and afobazole (1 mg/kg, i.p.) in comparison to fluoxetine (20 mg/kg, i.p.) and diazepam (1 mg/kg, i.p.) in open-field and marble burying tests on male mice of inbred strains BALB/C and C57BL/6. It is established that GIZh-72 administered both 30 min and 24 h before testing produces anxiolytic effect in the open-field test. The open field anxiety response patterns following GIZh-72 administration differed from these in diazepam or afobazole treated BALB/C mice. This drug also decreased the number of buried marbles in both BALB/C and C57BL/6 mice, the effect being comparable to that of afobazole and fluoxetine. In operant drug discrimination liquid-reinforcement paradigm in male Wistar rats, GIZh-72 failed to antagonize or substitute for the interoceptive stimulus cues of pentylenetetrazole evoking the saline-like responses in the latter case, which was evidence for the absence of properties of a ligand bearing positive modulator sites of GABA-A receptor.
2.[EVALUATION OF THE PHARMACOKINETIC INTERACTION OF AFOBAZOLE WITH CYP2C9 ENZYME DRUG SUBSTRATE OF CYTOCHROME P450].
Gribakina OG, Kolyvanov GB, Litvin AA, Smirnov VV, Shevchenko RV, Zherdev VP. Eksp Klin Farmakol. 2015;78(12):18-22.
We have studied the pharmacokinetics of drug-marker of cytochrome P450 isoenzyme CYP2C9 (losartan) and its metabolite E-3174 after subchronic oral administration of afobazole in doses 5 and 25 mg/kg in rats. The metabolic ratio (MR) of E-3174/Losartan was calculated. The pharmacokinetic parameters of losartan and its metabolite on the background of 4-day afabazole administration 5 mg/kg dose were not significantly different from analogous values calculated for the control group of rats. Therefore, afobazole in the effective anxiolytic dose did not change the MR value of metabolized P450 isoform. A five-fold dose increase in the afobazole dose led to significant difference in pharmacokinetic parameters, including A UC0-t, Cmax, Kel, t1/2el, MRT, CL/F, and Vd/F of losartan and AUC0-T, Cmax, and Tmax of E-3174. These findings are indicative of the induction of CYP2C9 isoenzyme by afobazole.
3.[Effect of L-carnitine, afobazole and their combination with L-arginine on biochemical and histological indices of endothelial disfunction in cobalt intoxication in rats].
Dzugkoev SG, Mozhaeva IV, Otiev MA, Margieva OI, Dzugkoeva FS. Patol Fiziol Eksp Ter. 2015 Apr-Jun;59(2):70-5.
The influence of L-carnitine and afobazole and their combination with L-arginine on biochemical and histological indices of endothelial dysfunction in rats with cobalt intoxication. The obtained data revealed biochemical markers of endothelial dysfunction. Found that-in rats with cobalt intoxication during treatment occurred inhibition of lipid peroxidation (LPO), reduced the concentration of malondialdehyde (MDA) in erythrocytes, activation of superoxide dismutase (SOD). This was accompanied by increased concentrations of nitric oxide (NO), the availability of the substrate L-arginine and possibly the expression of eNOS in the background of L-carnitine and afobazole.
4.Sigma-2 receptor ligands: neurobiological effects.
Guo L, Zhen X1. Curr Med Chem. 2015;22(8):989-1003.
Sigma-2 receptor is a widely distributed protein, which can modulate cell proliferation and involved in the pathogenesis of tumor. Photoaffinity labelling techniques testified that its molecular size is about 18 kDa. Recent studies indicated that sigma-2 receptor modulates the cytosolic Ca2+ concentration, dopaminergic transmission, and cocaine-induced addiction behavior. Some sigma-2 receptor ligands (ditolylguanidine, afobazole, etc) display the neuroprotective effect. Although sigma-2 receptor hasn't been cloned, tens of sigma-2 receptor ligands, which demonstrate high affinity and selectivity, have been identified in the past decade. In this review, we mainly focus on these series of selective sigma-2 receptor ligands, their neuropsychological effects, and molecular probes for tracing sigma-2 receptors in central nervous system.
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CAS 173352-21-1 Afobazole

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