| 词条 | Filaminast |
| 释义 |
| IUPAC_name = [(E)-1-(3-Cyclopentyloxy-4-methoxyphenyl)ethylideneamino] carbamate | image = Filaminast.svg | tradename = | pregnancy_category = | legal_status = Development terminated | routes_of_administration = | bioavailability = | metabolism = | elimination_half-life = | excretion = | CAS_number = 141184-34-1 | ATC_prefix = None | ATC_suffix = | PubChem = 9578243 | DrugBank = DB02660 | ChemSpiderID = 7852607 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = CDD69JC61J | KEGG = D04185 | C=15 | H=20 | N=2 | O=4 | molecular_weight = 292.33 g/mol | smiles = CC(=NOC(=O)N)C1=CC(=C(C=C1)OC)OC2CCCC2 }} Filaminast (code name WAY-PDA 641)[1] was a drug candidate developed by Wyeth-Ayerst.[2]{{rp|Table 2}} It is a phosphodiesterase 4 inhibitor (PDE4 inhibitor) and an analog of rolipram, which served as a prototype molecule for several development efforts.[3][4]{{rp|668, 678}} It was discontinued after a Phase II trial showed that its therapeutic window was too narrow; it could not be dosed high enough without causing significant side effects (nausea and vomiting), which was a problem with the rolipram class of molecules.[4]{{rp|678}} See also
References1. ^[https://pubchem.ncbi.nlm.nih.gov/compound/9578243?from=summary#section=Top Filaminist entry at Pubchem] {{Phosphodiesterase inhibitors}}{{Drugs for obstructive airway diseases}}2. ^Halpin DM. ABCD of the phosphodiesterase family: interaction and differential activity in COPD. Int J Chron Obstruct Pulmon Dis. 2008;3(4):543-61. {{PMID|19281073}} {{PMC|2650605}} 3. ^{{Cite journal|doi=10.1038/bjp.2008.297|pmc=2567889|pmid=18660832|title=Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking?|year=2008|last1=Giembycz|first1=M A|journal=British Journal of Pharmacology|volume=155|issue=3|pages=288–90}} 4. ^1 McKenna, JM and Muller, GW. Medicinal Chemistry of PDE4 Inhibitors. Chapter 33 in Cyclic Nucleotide Phosphodiesterases in Health and Disease, Eds Joseph A. Beavo et al. CRC Press, Dec 5, 2006 {{ISBN|9781420020847}} 4 : Abandoned drugs|Carbamates|PDE4 inhibitors|Phenol ethers |
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