Fenmetozole Tosylate 

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

Fenmetozole acts as an antagonist of α2-adrenergic receptor^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

417.31

C₁₇H₁₈Cl₂N₂O₄S

83474-08-2

ClC1=CC=C(OCC2=NCCN2)C=C1Cl.O=S(C3=CC=C(C)C=C3)(O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]