6-Br-APB

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6-Br-APB
(IUPAC) ime
3-alil-6-bromo-1-fenil-1,2,4,5-tetrahidro-3-benzazepin-7,8-diol
Klinički podaci
Identifikatori
CAS broj 135974-57-1
ATC kod nije dodeljen
PubChem[1][2] 11957483
ChemSpider[3] 8627436
ChEMBL[4] CHEMBL34095 YesY
Hemijski podaci
Formula C19H20BrNO2 
Mol. masa 374,27 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

6-Br-APB je sintetičko jedinjenje koje deluje kao selektivni agonist D1 receptora.[5] (R)-enantiomer je potentan pun agonist, dok (S) enantiomer ima D1 selektivnost, ali je slab parcijalni agonist.[6] (R)-6-Br-APB i slični D1-selektivni puni agonisti, kao što su SKF-81297 i SKF-82958 proizvode karakteristične anoreksične efekte, stereotipno ponašanje i samoadministraciju kod životinja. On ima sličan mada ne identičan profile sa dopaminergičkim stimulansima poput amfetamina.[7][8][9]

Reference[uredi - уреди | uredi izvor]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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 Chemistry 4: 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 Cheminform 2 (1): 3. PMID 20331846. doi:10.1186/1758-2946-2-3.  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 Res 40 (Database issue): D1100–7. PMID 21948594. doi:10.1093/nar/gkr777.  edit
  5. Neumeyer JL, Baindur N, Niznik HB, Guan HC, Seeman P (December 1991). "(+/-)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3- benzazepin, a new high-affinity D1 dopamine receptor ligand: synthesis and structure-activity relationship". Journal of Medicinal Chemistry 34 (12): 3366–71. PMID 1684995. doi:10.1021/jm00116a004. 
  6. Neumeyer JL, Kula NS, Baldessarini RJ, Baindur N (April 1992). "Stereoisomeric probes for the D1 dopamine receptor: synthesis and characterization of R-(+) and S-(-) enantiomers of 3-allyl-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine and its 6-bromo analogue". Journal of Medicinal Chemistry 35 (8): 1466–71. PMID 1533424. doi:10.1021/jm00086a016. 
  7. Rosenzweig-Lipson S, Hesterberg P, Bergman J (September 1994). "Observational studies of dopamine D1 and D2 agonists in squirrel monkeys". Psychopharmacology 116 (1): 9–18. PMID 7862937. doi:10.1007/BF02244865. 
  8. Weed MR, Woolverton WL (December 1995). "The reinforcing effects of dopamine D1 receptor agonists in rhesus monkeys". The Journal of Pharmacology and Experimental Therapeutics 275 (3): 1367–74. PMID 8531104. 
  9. Barrett AC, Miller JR, Dohrmann JM, Caine SB (2004). "Effects of dopamine indirect agonists and selective D1-like and D2-like agonists and antagonists on cocaine self-administration and food maintained responding in rats". Neuropharmacology. 47 Suppl 1: 256–73. PMID 15464142. doi:10.1016/j.neuropharm.2004.07.007. 


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