Name Carmoterol powder
Chemical name 2(1H)-Quinolinone, 8-hydroxy-5-(1-hydroxy-2-((2-(4-methoxyphenyl)-1-methylethyl)amino)ethyl)-, (R-(R*,R*))-
Synonyms Carmoterol ; CHF 4226; UNII-9810NUL4D1; Carmoterol [INN].
Molecular Formula C21H24N2O4
Molecular Weight 368.433 g/mol
Melting Point Unknow
InChI Key IHOXNOQMRZISPV-YJYMSZOUSA-N
Appearance Light Beige to Beige
Half Life Unknow
Solubility Soluble in Methanol (Slightly)
Storage Condition Refrigerator, Under Inert Atmosphere
Application Carmoterol is a highly potent β2-selective adrenoceptor agonist having a long-lasting bronchodilatingeffect.
Testing Document Available
03 Carmoterol powder (147568-66-9) General Description
Carmoterol, this agent has a rapid onset, is a selective (RR) pure isomer, and is a full beta2-agonist — which is in phase 2 clinical development as a hydrofluoroalkane pMDI with Chiesi’s proprietary modulite technology.This agent is also being developed as a fixed combination with an inhaled corticosteroid, and it is stable for at least 18 months at room temperature. The pharmacologic profile of carmoterol includes the fact that its potency in isolated guinea pig trachea is greater than formoterol and salmeterol. It is over 100 times more selective for bronchial muscle than myocardial tissue. This agent has been studied in healthy volunteers and in asthmatic patients with multiple escalating doses; there were no dose-response effects on glucose level and serum potassium, and very little tremor occurred except at the highest doses of 12-16 micrograms (mcg). Clinically, 2 mcg seems like the appropriate dose. No significant differences occurred in the QTc interval or in heart rate. Prof. Bousquet, from France, concluded that once-daily carmoterol demonstrated 24-hour bronchodilating effects. All doses had a rapid onset of action. Doses from 1.5 to 3 mcg produced clinically meaningful increases in forced expiratory volume in 1 second (FEV1), which persisted for 24 hours. In all doses tested, carmoterol was well tolerated with a good safety profile and no clinically relevant systemic effects.
04 Carmoterol powder (147568-66-9) History
Carmoterol (INN), also known as TA-2005 and CHF-4226, is a non-catechol experimental ultra-long-acting β adrenoreceptor agonist (ultra-LABA)that was in clinical trials before 2010 when it has been withdrawn fromfurther development based on evidence that the compound does not possess a competitive profile
Preliminary studies indicated duration of its effect exceeding 24 hours after inhalation of 3 μg.The pharmacologic profile of this medication included the fact its potency in isolated guinea pig trachea is greater than that of formoterol and salmeterol. It is over 100 times more selective for bronchial muscle than myocardial tissue.