| 词条 | LG-120907 |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = 2,2-Dimethyl-6-(trifluoromethyl)-1,9-dihydropyrido[3,2-g]quinolin-8-one | image = LG-120907.svg | width = | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | class = Nonsteroidal antiandrogen | CAS_number_Ref = | CAS_number = | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 10851308 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 9026602 | UNII = | KEGG = | ChEBI = | ChEMBL = 350877 | synonyms = 1,2,3,4-Tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quinoline | C=15 | H=13 | F=3 | N=2 | O=1 | molecular_weight = 294.277 g/mol | SMILES = CC1(C=CC2=C(N1)C=C3C(=C2)C(=CC(=O)N3)C(F)(F)F)C | StdInChI_Ref = | StdInChI = 1S/C15H13F3N2O/c1-14(2)4-3-8-5-9-10(15(16,17)18)6-13(21)19-12(9)7-11(8)20-14/h3-7,20H,1-2H3,(H,19,21) | StdInChIKey_Ref = | StdInChIKey = MMLSXRYBGYGQEP-UHFFFAOYSA-N }}LG-120907 is a nonsteroidal antiandrogen (NSAA) of the quinoline group which was developed by Ligand Pharmaceuticals along with selective androgen receptor modulators (SARMs) like LG-121071 and was never marketed.[1][2][3][4] The drug is a high-affinity antagonist of the androgen receptor (AR) with a Ki value of 26 nM and has been found to inhibit growth of the ventral prostate and seminal vesicles in male rats without increasing circulating levels of luteinizing hormone or testosterone.[1][2][3] However, this tissue selectivity has not been assessed in humans.[5] LG-120907 is orally active and shows greater oral potency than the arylpropionamide NSAA flutamide.[1][3][4] The 7-fluoro derivative of LG-120907, LG-105, is also a potent NSAA, and appears to possess greater potency in comparison.[3] Conversely, the 6-ethyl, 8-didesmethyl analogue of LG-120907, LG-121071, is a SARM with potent androgenic activity equivalent to that of dihydrotestosterone (DHT).[1][3] References1. ^1 2 3 {{cite journal|last1=Chengalvala|first1=Murty|last2=Oh|first2=Thomas|last3=Roy|first3=Arun K|title=Selective androgen receptor modulators|journal=Expert Opinion on Therapeutic Patents|volume=13|issue=1|year=2005|pages=59–66|issn=1354-3776|doi=10.1517/13543776.13.1.59}} {{Androgen receptor modulators}}{{genito-urinary-drug-stub}}2. ^1 {{cite journal|last1=Mohler|first1=Michael L|last2=Nair|first2=Vipin A|last3=Hwang|first3=Dong Jin|last4=Rakov|first4=Igor M|last5=Patil|first5=Renukadevi|last6=Miller|first6=Duane D|title=Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates|journal=Expert Opinion on Therapeutic Patents|volume=15|issue=11|year=2005|pages=1565–1585|issn=1354-3776|doi=10.1517/13543776.15.11.1565}} 3. ^1 2 3 4 {{cite journal | vauthors = Gao W, Kim J, Dalton JT | title = Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands | journal = Pharm. Res. | volume = 23 | issue = 8 | pages = 1641–58 | year = 2006 | pmid = 16841196 | pmc = 2072875 | doi = 10.1007/s11095-006-9024-3 | url = }} 4. ^1 {{cite journal | vauthors = Nyrönen TH, Söderholm AA | title = Structural basis for computational screening of non-steroidal androgen receptor ligands | journal = Expert Opin Drug Discov | volume = 5 | issue = 1 | pages = 5–20 | year = 2010 | pmid = 22823968 | doi = 10.1517/17460440903468680 | url = }} 5. ^{{cite book|author=Rob Bradbury|title=Cancer|url=https://books.google.com/books?id=fdtDAAAAQBAJ&pg=PA67|date=30 January 2007|publisher=Springer Science & Business Media|isbn=978-3-540-33120-9|pages=67–}} 5 : Ketones|Nonsteroidal antiandrogens|Pyridines|Quinolines|Trifluoromethyl compounds |
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