ChemicalBook--->CAS DataBase List--->147568-66-9

147568-66-9

147568-66-9 Structure

147568-66-9 Structure
IdentificationBack Directory
[Name]

8-hydroxy-5-[1-hydroxy-2-[2-(4-methoxyphenyl)propan-2-ylamino]ethyl]-1H-quinolin-2-one
[CAS]

147568-66-9
[Synonyms]

C Motro
CHF 4226
Carmoterol
CarMotelrol
Carmoterol and its intermediates
8-hydroxy-5-[1-hydroxy-2-[2-(4-methoxyphenyl)propan-2-ylamin...
8-hydroxy-5-[1-hydroxy-2-[2-(4-methoxyphenyl)propan-2-ylamino]ethyl]-1H-quinolin-2-one
8-Hydroxy-5-((R)-1-hydroxy-2-(((R)-1-(4-Methoxyphenyl)propan-2-yl)aMino)ethyl)quinolin-2(1H)-one
8-Hydroxy-5-[(R)-1-hydroxy-2-[[(R)-1-methyl-2-(4-methoxyphenyl)ethyl]amino]ethyl]quinolin-2(1H)-one
8-Hydroxy 5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-2(1H)-quinolinone
2(1h)-quinolinone, 8-hydroxy-5-[(1r)-1-hydroxy-2-[[(1r)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]-
8-Hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-Methoxyphenyl)-1-Methylethyl]aMino]ethyl]-2(1H)-quinolinone CarMoterol
[EINECS(EC#)]

1312995-182-4
[Molecular Formula]

C21H24N2O4
[MDL Number]

MFCD16621079
[MOL File]

147568-66-9.mol
[Molecular Weight]

368.43
Chemical PropertiesBack Directory
[Boiling point ]

649.1±55.0 °C(Predicted)
[density ]

1.248
[storage temp. ]

Keep in dark place,Inert atmosphere,Room temperature
[pka]

8.68±0.20(Predicted)
Hazard InformationBack Directory
[Uses]

Carmoterol is a highly potent, selective and long-acting β2-adrenoceptor agonist with the pEC50 of 10.19. Carmoterol has 53 times higher affinity for the β2-adrenoceptors than for the β1-adrenoceptors[1][2]. Carmoterol can be used for the research of asthma and chronic obstructive pulmonary disease (COPD)[2].
[in vivo]

Bronchoconstriction is induced in normal guinea-pigs by intravenous administration of graded doses of Acetylcholine (10, 20 and 40 mg/kg) and Histamine (5, 10 and 20 mg/kg) or in actively sensitized animals by Ovalbumin (5 mg/kg). Carmoterol (from 0.3 to 100 pmol) is given by superfusion onto the tracheal mucosa for 5 min before challenge. Carmoterol causes a dose-dependent inhibition of the acetylcholine-induced bronchoconstriction with the ED50 of 16.7 pmol[2].

Animal Model:Male Dunkin Hartley guinea-pigs (weighing 360-380 g)[2]
Dosage:0.3 to 100 pmol.
Administration:Given by superfusion (0.01 mL/min) onto the tracheal mucosa for 5 min before challenge.
Result:Caused a dose-dependent inhibition of the Acetylcholine-induced bronchoconstriction.
Was very potent against Histamine and Ovalbumin-induced reaction, being effective already at 1 pmol.
[References]

[1] Mario Cazzola, et al. β(2) -adrenoceptor agonists: current and future direction. Br J Pharmacol. 2011 May;163(1):4-17. DOI:10.1111/j.1476-5381.2011.01216.x
[2] Giuseppe Rossoni, et al. Positive interaction of the novel beta2-agonist carmoterol and tiotropium bromide in the control of airway changes induced by different challenges in guinea-pigs. Pulm Pharmacol Ther. 2007;20(3):250-7. DOI:10.1016/j.pupt.2006.01.004
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