A-86929

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A-86929
IUPAC ime
Identifikacija
CAS registarski broj 166591-11-3DaY
PubChem[1][2] 9841398
ChemSpider[3] 8017113DaY
ChEMBL[4] CHEMBL28338DaY
Jmol-3D slike Slika 1
Svojstva
Molekulska formula C18H21NO2S
Molarna masa 315,429 g/mol

DaY(šta je ovo?) (verifikuj)

Ukoliko nije drugačije napomenuto, podaci se odnose nastandardno stanje (25 °C, 100 kPa)materijala

Infobox references

A-86929je sintetičko jedinjenje koje deluje kao selektivniagonistdopaminskog receptoraD1.[5][6]On je razvijen kao mogući treatment zaParkinsonovu bolest,[7]kao i za druge primene, poput kokainske adikcije.[8][9]On ima relativno dobru efikasnost na ljudima, međutim uzrokujediskinezije,te je njegov razvoj prekinut.[10][11]On je uglavnom korišten u obliku diacetatnogestra,prolekaadrogolid(ABT-431), koji ima boljubiodostupnost.[12][13]

Adrogolid

Reference

[uredi|uredi kod]
  1. ↑Li Q, Cheng T, Wang Y, Bryant SH (2010).„PubChem as a public resource for drug discovery.”.Drug Discov Today15(23-24): 1052-7.DOI:10.1016/j.drudis.2010.10.003.PMID20970519.edit
  2. ↑Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”.Annual Reports in Computational Chemistry4:217-241.DOI:10.1016/S1574-1400(08)00012-1.
  3. ↑Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010).„Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”.J Cheminform2(1): 3.DOI:10.1186/1758-2946-2-3.PMID20331846.edit
  4. ↑Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”.Nucleic Acids Res40(Database issue): D1100-7.DOI:10.1093/nar/gkr777.PMID21948594.edit
  5. ↑Michaelides MR, Hong Y, DiDomenico S, Asin KE, Britton DR, Lin CW, Williams M, Shiosaki K (September 1995). „(5aR,11bS)-4,5,5a,6,7,11b-hexahydro-2-propyl-3-thia-5-azacyclopent-1- ena[c]-phenanthrene-9,10-diol (A-86929): a potent and selective dopamine D1 agonist that maintains behavioral efficacy following repeated administration and characterization of its diacetyl prodrug (ABT-431)”.Journal of Medicinal Chemistry38(18): 3445–7.DOI:10.1021/jm00018a002.PMID7658429.
  6. ↑Ehrlich PP, Ralston JW, Michaelides MR (May 1997). „An Efficient Enantioselective Synthesis of the D1 Agonist (5aR,11bS)-4,5,5a,6,7,11b-Hexahydro-2-propyl-3-thia- 5-azacyclopenta[c]phenanthrene-9,10-diol (A-86929)”.The Journal of Organic Chemistry62(9): 2782–2785.DOI:10.1021/jo970066l.PMID11671640.
  7. ↑Rascol O, Blin O, Thalamas C, Descombes S, Soubrouillard C, Azulay P, Fabre N, Viallet F, Lafnitzegger K, Wright S, Carter JH, Nutt JG (June 1999).„ABT-431, a D1 receptor agonist prodrug, has efficacy in Parkinson's disease”.Annals of Neurology45(6): 736–41.DOI:10.1002/1531-8249(199906)45:6<736::AID-ANA7>3.0.CO;2-F.PMID10360765.
  8. ↑Haney M, Collins ED, Ward AS, Foltin RW, Fischman MW (March 1999).„Effect of a selective dopamine D1 agonist (ABT-431) on smoked cocaine self-administration in humans”.Psychopharmacology143(1): 102–10.DOI:10.1007/s002130050925.PMID10227086.
  9. ↑Gorelick DA, Gardner EL, Xi ZX (2004). „Agents in development for the management of cocaine abuse”.Drugs64(14): 1547–73.DOI:10.2165/00003495-200464140-00004.PMID15233592.
  10. ↑Rascol O, Nutt JG, Blin O, Goetz CG, Trugman JM, Soubrouillard C, Carter JH, Currie LJ, Fabre N, Thalamas C, Giardina WW, Wright S (February 2001). „Induction by dopamine D1 receptor agonist ABT-431 of dyskinesia similar to levodopa in patients with Parkinson disease”.Archives of Neurology58(2): 249–54.DOI:10.1001/archneur.58.2.249.PMID11176963.
  11. ↑Zhang J, Xiong B, Zhen X, Zhang A (March 2009). „Dopamine D1 receptor ligands: where are we now and where are we going”.Medicinal Research Reviews29(2): 272–94.DOI:10.1002/med.20130.PMID18642350.
  12. ↑Shiosaki K, Jenner P, Asin KE, Britton DR, Lin CW, Michaelides M, Smith L, Bianchi B, Didomenico S, Hodges L, Hong Y, Mahan L, Mikusa J, Miller T, Nikkel A, Stashko M, Witte D, Williams M (January 1996). „ABT-431: the diacetyl prodrug of A-86929, a potent and selective dopamine D1 receptor agonist: in vitro characterization and effects in animal models of Parkinson's disease”.The Journal of Pharmacology and Experimental Therapeutics276(1): 150–60.PMID8558425.
  13. ↑Giardina WJ, Williams M (2001). „Adrogolide HCl (ABT-431; DAS-431), a prodrug of the dopamine D1 receptor agonist, A-86929: preclinical pharmacology and clinical data”.CNS Drug Reviews7(3): 305–16.DOI:10.1111/j.1527-3458.2001.tb00201.x.PMID11607045.
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