Arformoterol Tartrate

Research use only, not for human use.

Arformoterol Tartrate is the tartrate salt of arformoterol. Arformoterol is a long-acting beta-2 adrenergic agonist with bronchodilator activity.

Arformoterol Tartrate is the tartrate salt of arformoterol. Arformoterol is a long-acting beta-2 adrenergic agonist with bronchodilator activity.(In Vivo):Arformoterol (R,R-formoterol) is a active isomer of racemic formoterol and is indicated for the long-term, maintenance treatment of bronchoconstriction in patients with COPD including chronic bronchitis and emphysema. It is a potent and selective agent which causes bronchial smooth muscle relaxation and inhibits the release of inflammatory mediators. Its pharmacological effects can be attributed to the increased intracellular cyclic adenosine monophosphate (cAMP) levels that result from the stimulation of intracellular adenyl cyclase. Arformoterol tartrate is well absorbed through lungs when administered by a nebulizer. The mean peak plasma concentration (Cmax) and systemic exposure (AUC0-12h) are 4.3 pg/mL and 34.5 pg.h/mL, respectively, when 15 μg arformoterol is administered every 12 h for 14 days in COPD patients. The time to achieve median steady state peak plasma concentration (tmax) is approximately half an hour after drug administration. The mean terminal half-life is 26 h in COPD patients when treated with 15 μg inhaled arformoterol twice daily for 14 days. The binding of arformoterol to human plasma proteins in vitro is 52-65% at concentrations of 0.25, 0.5 and 1.0 ng/mL of radiolabeled arformoterol. Metabolism occurs primarily by direct conjugation (glucuronidation) and secondary route of metabolism is via O-demethylation. Metabolism is mediated by atleast five human uridine diphosphoglucuronosyltransferase (UGT) isozymes as well as CYP2D6 and CYP2C19. After administration of a single oral dose of radiolabeled arformoterol, 63% of the radioactive amount was recovered in urine and 11% in feces within 48 h. A total of 89% of the total radioactive dose was recovered within 14 days, with 67% in urine and 22% in faeces.

Arformoterol tartrate induces cAMP accumulation in cultured human bronchial epithelial cells.

Arformoterol tartrate (10 ng in 0.1 ml saline/20 g body weight; intranasal instillation) mitigates Cl2-induced increases of respiratory system resistance and elastance in mice.Arformoterol tartrate reverses histamine- and ovalbumin-induced bronchoconstriction in guinea pigs (ED50s=1 and 40 nmol/kg, respectively). Animal Model:Wild-type and iNOS?/? mice were exposed to Cl2 gas Dosage:10 ng in 0.1 ml saline/20 g body weight Administration: Intranasal instillation in the external nares at 10 minutes and every 24 hours after exposure Result:Significantly mitigated the Cl2-induced increases of respiratory system resistance and elastance. Increased cAMP in the lungs of Cl2-exposed mice.Not mitigated Cl2-induced lung injury and inflammation.

(R,R)-Formoterol tartrate

Angiogenesis

Adrenergic Receptor

Xanthine oxidase|Endogenous Metabolite

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200815-49-2

494.497

C23H30N2O10

>98% (HPLC)

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O[C@H]([C@@H](O)C(O)=O)C(O)=O.COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1

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(-20℃)

With Ice Pack

≥ 2 years