Fluparoxan  (Synonyms: GR50360)

Fluparoxan is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan is an anti-depressant agent^[1][2].

In the rat isolated, field-stimulated vas deferens and the guinea-pig isolated, field-stimulated ileum preparations, Fluparoxan is a reversible competitive antagonist of the inhibitory responses to the alpha 2-adrenoceptor agonist UK-14304 (HY-B0659) with pKB values of 7.87 and 7.89 respectively^[1].
In the rat isolated anococcygeus muscle, Fluparoxan is a much weaker competitive antagonist of the contractile response to the alpha 1-adrenoceptor agonist phenylephrine (HY-B0769) with a pKB of 4.45 giving an alpha 2: alpha 1-adrenoceptor selectivity ratio of greater than 2500^[1].

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

In the conscious mouse, Fluparoxan (0.2-3.0 mg/kg) is effective by the oral route and of similar potency to idazoxan (HY-14561) in preventing clonidine (HY-12721)-induced hypothermia and antinociception^[1].
Fluparoxan (0.67-6 mg/kg, p.o.) prevents UK-14304 (HY-B0659)-induced sedation and bradycardia in the dog^[1].

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

195.19

C₁₀H₁₀FNO₂

105182-45-4

FC1=C2C(O[C@]3([H])[C@@](CNC3)([H])O2)=CC=C1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Halliday CA, et al. The pharmacology of fluparoxan: a selective alpha 2-adrenoceptor antagonist. Br J Pharmacol. 1991 Apr;102(4):887-95.  [Content Brief]

  [2]. Altria K D .High and low injection volumes in CE for improved quantitative determination of drug related impurities[J].Chromatographia, 1993, 35(9):493-496.