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83474-08-2

83474-08-2 Structure

83474-08-2 Structure
IdentificationBack Directory
[Name]

Fenmetozole (Tosylate)
[CAS]

83474-08-2
[Synonyms]

Fenmetozole (Tosylate)
[Molecular Formula]

C17H18Cl2N2O4S
[MDL Number]

MFCD31544467
[MOL File]

83474-08-2.mol
[Molecular Weight]

417.307
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
Hazard InformationBack Directory
[Uses]

Fenmetozole Tosylate is an antagonist of the actions of ethanol, also antagonizes α2-adrenergic receptor, and acts as an antidepressant agent.
[in vivo]

In mice, fenmetozole antagonizes both the ethanol induced increase in locomotor activity at 2.0 g/kg and the decrease caused by 4.0 g/kg. Moreover, fenmetozole attenuates the ethanol-induced reduction in cerebellar cyclic guanosine monophosphate content, but it significantly elevates cGMP levels in this tissue. Fenmetozole does not change ethanol induced increases in punished drinking in a conflict test, but when given at a high dose, fenmetozole decreases both punished and unpunished responding. Fenmetozole fails to precipitate ethanol withdrawal-like reactions when it is given to physically-dependent, intoxicated rats. Fenmetozole (15-30 g/kg) reduces ethanol-induced impairment of the aerial righting reflex without altering blood or brain ethanol content[1]. Fenmetozole alone has no ffect on punished drinking and does not alter ethanol action in the paradigm except at the highest dose tested (30 mg/kg) in rats[2].

[IC 50]

α adrenergic receptor
[storage]

Store at -20°C
[References]

[1] Frye GD, et al. An evaluation of the selectivity of fenmetozole (DH-524) reversal of ethanol-induced changes in central nervous system function. Psychopharmacology (Berl). 1980;69(2):149-55. DOI:10.1007/BF00427641
[2] Vogel RA, et al. Differential effects of TRH, amphetamine, naloxone, and fenmetozole on ethanol actions: attenuation of the effects of punishment and impairment of aerial righting reflex. Alcohol Clin Exp Res. 1981 Summer;5(3):386-92. DOI:10.1111/j.1530-0277.1981.tb04921.x
[3] Stillings MR, et al. Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists. J Med Chem. 1986 Sep;29(9):1780-3. DOI:10.1021/jm00159a037
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