| 词条 | Andarine |
| 释义 |
| Verifiedfields = changed | verifiedrevid = 457130171 | IUPAC_name = (2S)-3-(4-acetamido-phenoxy)-2-hydroxy-2-methyl-N-(4-nitro-3-trifluoromethyl-phenyl)-propionamide | image = Andarine.svg | width = 250px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = Investigational New Drug | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | IUPHAR_ligand = 7849 | CAS_number_Ref = {{cascite|changed|??}} | CAS_number = 401900-40-1 | ATC_prefix = None | ATC_suffix = | ATC_supplemental = | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 125236 | PubChem = 9824562 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 8000309 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB07423 | synonyms = Acetamidoxolutamide; Androxolutamide; GTx-007; S-4 | C=19 | H=18 | F=3 | N=3 | O=6 | molecular_weight = 441.357 g/mol | SMILES = FC(F)(F)c1cc(ccc1[N+]([O-])=O)NC(=O)[C@@](O)(COc2ccc(cc2)NC(=O)C)C | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C19H18F3N3O6/c1-11(26)23-12-3-6-14(7-4-12)31-10-18(2,28)17(27)24-13-5-8-16(25(29)30)15(9-13)19(20,21)22/h3-9,28H,10H2,1-2H3,(H,23,26)(H,24,27)/t18-/m0/s1 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = YVXVTLGIDOACBJ-SFHVURJKSA-N }}Andarine (developmental code names GTx-007, S-4) is an investigational selective androgen receptor modulator (SARM) developed by GTX, Inc for treatment of conditions such as muscle wasting, osteoporosis and benign prostatic hypertrophy,[1] using the nonsteroidal antiandrogen bicalutamide as a lead compound.[2] Andarine is an orally active partial agonist of the androgen receptor (AR). It is less potent in both anabolic and androgenic effects than other SARMs. In an animal model of benign prostatic hypertrophy, andarine was shown to reduce prostate weight with similar efficacy to finasteride, but without producing any reduction in muscle mass or antiandrogenic side effects.[3] This suggests that it is able to competitively block binding of dihydrotestosterone to its receptor targets in the prostate gland, but its partial agonist actions at the AR prevent the side effects associated with the antiandrogens traditionally used for treatment of BPH.[4] See also
References1. ^{{cite journal | vauthors = Hott JL, Borkman RF | title = The non-fluorescence of 4-fluorotryptophan | journal = The Biochemical Journal | volume = 264 | issue = 1 | pages = 297–9 | date = November 1989 | pmid = 2604714 | pmc = 1133577 | doi = 10.1124/jpet.102.040840 }} {{Androgen receptor modulators}}{{Antineoplastic-drug-stub}}{{Genito-urinary-drug-stub}}2. ^{{cite journal | vauthors = Chen J, Kim J, Dalton JT | title = Discovery and therapeutic promise of selective androgen receptor modulators | journal = Molecular Interventions | volume = 5 | issue = 3 | pages = 173–88 | date = June 2005 | pmid = 15994457 | pmc = 2072877 | doi = 10.1124/mi.5.3.7 }} 3. ^G{{cite journal | vauthors = Gao W, Kearbey JD, Nair VA, Chung K, Parlow AF, Miller DD, Dalton JT | title = Comparison of the pharmacological effects of a novel selective androgen receptor modulator, the 5alpha-reductase inhibitor finasteride, and the antiandrogen hydroxyflutamide in intact rats: new approach for benign prostate hyperplasia | journal = Endocrinology | volume = 145 | issue = 12 | pages = 5420–8 | date = December 2004 | pmid = 15308613 | pmc = 2098692 | doi = 10.1210/en.2004-0627 }} 4. ^{{cite journal | vauthors = Gao W, Kim J, Dalton JT | title = Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands | journal = Pharmaceutical Research | volume = 23 | issue = 8 | pages = 1641–58 | date = August 2006 | pmid = 16841196 | pmc = 2072875 | doi = 10.1007/s11095-006-9024-3 }} 4 : Carboxamides|Phenol ethers|Selective androgen receptor modulators|Trifluoromethyl compounds |
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