SB-216641

SB-216641
Systematic (IUPAC) name
N-[3-[3-(dimethylamino)ethoxy]-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide
Clinical data
Identifiers
170230-39-4 Yes
None
PubChem CID 3292447
IUPHAR ligand 28
Chemical data
Formula C28H30N4O4
486.561 g/mol
 Yes (what is this?)  (verify)

SB-216641 is a drug which is a selective antagonist for the serotonin receptor 5-HT1B, with around 25x selectivity over the closely related 5-HT1D receptor.[1] It is used in scientific research,[2][3][4] and has demonstrated anxiolytic effects in animal studies.[5][6]

References

  1. ↑ Price, GW; Burton, MJ; Collin, LJ; Duckworth, M; Gaster, L; Göthert, M; Jones, BJ; Roberts, C et al. (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. doi:10.1007/PL00005056. PMID 9303567.
  2. ↑ 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. doi:10.1016/j.neures.2003.11.004. PMID 15154669.
  3. ↑ 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. doi:10.1016/j.brainres.2004.06.053. PMID 15328035.
  4. ↑ 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. doi:10.1038/sj.npp.1301396. PMID 17392733.
  5. ↑ 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. doi:10.1097/00008877-200412000-00001. PMID 15577451.
  6. ↑ 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. doi:10.1211/0022357055399. PMID 15720791.