Fluparoxan


CAS No. : 105182-45-4

(Synonyms: GR50360)

105182-45-4
Price and Availability of CAS No. : 105182-45-4
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Cat. No. : HY-106769
M.Wt: 195.19
Formula: C10H10FNO2
Purity: >98 %
Solubility: 10 mM in DMSO
Introduction of 105182-45-4 :

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

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