SB-216,641

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SB-216,641
(IUPAC) ime
N-[3-[3-(dimetilamino)etoksi]-4-metoksifenil]-2'-metil-4'-(5-metil-1,2,4-oksadiazol-3-il)-[1,1'-bifenil]-4-karboksamid
Klinički podaci
Identifikatori
CAS broj 170230-39-4
ATC kod nije dodeljen
PubChem[1][2] 3292447
Hemijski podaci
Formula C28H30N4O4 
Mol. masa 486,561 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

SB-216,641 je lek, koji je selektivni antagonist za serotoninski receptor 5-HT1B, sa oko 25x većom selektivnošću u odnosu na srodni 5-HT1D receptor.[3] On se koristi u naučnim istraživanjima,[4][5][6] i pokazano je da ima anksiolitsko dejstvo u životinjskim studijama.[7][8]

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. Price, GW; Burton, MJ; Collin, LJ; Duckworth, M; Gaster, L; Göthert, M; Jones, BJ; Roberts, C; Watson, JM (1997). "SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors". Naunyn-Schmiedeberg's archives of pharmacology 356 (3): 312–20. PMID 9303567. doi:10.1007/PL00005056. 
  4. Matsuoka, T; Hasuo, H; Akasu, T (2004). "5-Hydroxytryptamine 1B receptors mediate presynaptic inhibition of monosynaptic IPSC in the rat dorsolateral septal nucleus". Neuroscience research 48 (3): 229–38. PMID 15154669. doi:10.1016/j.neures.2003.11.004. 
  5. Yan, QS; Zheng, SZ; Yan, SE (2004). "Involvement of 5-HT1B receptors within the ventral tegmental area in regulation of mesolimbic dopaminergic neuronal activity via GABA mechanisms: a study with dual-probe microdialysis". Brain Research 1021 (1): 82–91. PMID 15328035. doi:10.1016/j.brainres.2004.06.053. 
  6. Lee, JJ; Hahm, ET; Lee, CH; Cho, YW (2008). "Serotonergic modulation of GABAergic and glutamatergic synaptic transmission in mechanically isolated rat medial preoptic area neurons". Neuropsychopharmacology 33 (2): 340–52. PMID 17392733. doi:10.1038/sj.npp.1301396. 
  7. Tatarczyńska, E; Kłodzińska, A; Stachowicz, K; Chojnacka-Wójcik, E (2004). "Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression". Behavioural Pharmacology 15 (8): 523–34. PMID 15577451. doi:10.1097/00008877-200412000-00001. 
  8. Chojnacka-Wójcik, E; Kłodzińska, A; Tatarczyńska, E (2005). "The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action". The Journal of pharmacy and pharmacology 57 (2): 253–7. PMID 15720791. doi:10.1211/0022357055399. 

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