词条 | Carmoterol |
释义 |
| Watchedfields = changed | verifiedrevid = | IUPAC_name = 8-hydroxy-5-[(1R)-1-hydroxy-2-[[(2R)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]-1H-quinolin-2-one | image = Carmoterol.svg | width = 255 | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | routes_of_administration = Inhalation | legal_status = Development terminated | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = | ATC_prefix = None | ATC_suffix = | PubChem = 63952 | IUPHAR_ligand = | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 57545 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 9810NUL4D1 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1094785 | C=21 | H=24 | N=2 | O=4 | smiles = COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3NC(=O)C=Cc23)cc1 | StdInChI = 1S/C21H24N2O4/c1-13(11-14-3-5-15(27-2)6-4-14)22-12-19(25)16-7-9-18(24)21-17(16)8-10-20(26)23-21/h3-10,13,19,22,24-25H,11-12H2,1-2H3,(H,23,26)/t13-,19+/m1/s1 | StdInChIKey = IHOXNOQMRZISPV-YJYMSZOUSA-N }}Carmoterol ({{w|International nonproprietary name|INN}}),[1] also known as TA-2005 and CHF-4226, is a non-catechol[2] experimental ultra-long-acting β adrenoreceptor agonist (ultra-LABA)[2][3] that was in clinical trials before 2010 when it has been withdrawn from further development based on evidence that the compound does not possess a competitive profile.[4] Preliminary studies indicated duration of its effect exceeding 24 hours after inhalation of 3 μg.[2] 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.[5] References1. ^{{cite journal|title=International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 53|journal=WHO Drug Information|date=2005|volume=19|issue=1|page=74|url=http://www.who.int/medicines/publications/druginformation/innlists/RL53.pdf|accessdate=25 March 2016}} {{Adrenergic agonists}}{{Asthma and copd rx}}{{respiratory-system-drug-stub}}2. ^1 2 {{cite book|last1=Mario, MD, MPH|first1=Castro|last2=Monica, MD|first2=Kraft|title=Clinical Asthma|date=2008|publisher=Mosby / Elsevier Health Sciences|location=1600 John F. Kennedy Boulevard, Suite 1800, Philadelphia, PA 19103–2899|isbn=978-0-323-04289-5|chapter=27. Bronchodilators: Beta2-Agonists and Anticholingercs}} 3. ^{{cite journal|last1=Cazzola|first1=Mario|last2=Calzetta|first2=Luigino|last3=Matera|first3=Maria Gabriella|title=β2-adrenoceptor agonists: current and future direction|journal=British Journal of Pharmacology|date=May 2011|volume=163|issue=1|pages=4–17|doi=10.1111/j.1476-5381.2011.01216.x|pmid=21232045|pmc=3085864}} 4. ^{{cite web|title=Chiesi: Annual Report 2010|url=http://www.chiesi.es/Assets/docs/Annual_report_2010.pdf|publisher=Chiesi Farmaceutici S.p.A.|accessdate=27 March 2016|page=20}} 5. ^{{cite journal|last1=Donohue, MD|first1=James F|title=New Options in COPD Therapy|journal=Medscape|date=2006|url=http://www.medscape.com/viewarticle/547182|accessdate=27 March 2016}} 6 : Abandoned drugs|Long-acting beta2-adrenergic agonists|2-Quinolones|Quinolinols|Secondary alcohols|Phenol ethers |
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