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SB-216,641
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
Identifiers
CAS number 170230-39-4
ATC code  ?
PubChem 3292447
Chemical data
Formula C 28H30N4O4  
Mol. mass 486.561 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

SB-216,641 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, Watson JM, Middlemiss DN. SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Archives of Pharmacology. 1997 Sep;356(3):312-20. PMID 9303567
  2. ^ Matsuoka T, Hasuo H, Akasu T. 5-Hydroxytryptamine 1B receptors mediate presynaptic inhibition of monosynaptic IPSC in the rat dorsolateral septal nucleus. Neuroscience Research. 2004 Mar;48(3):229-38. PMID 15154669
  3. ^ Yan QS, Zheng SZ, Yan SE. 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. 2004 Sep 17;1021(1):82-91. PMID 15328035
  4. ^ Lee JJ, Hahm ET, Lee CH, Cho YW. Serotonergic modulation of GABAergic and glutamatergic synaptic transmission in mechanically isolated rat medial preoptic area neurons. Neuropsychopharmacology. 2008 Jan;33(2):340-52. PMID 17392733
  5. ^ Tatarczyńska E, Kłodzińska A, Stachowicz K, Chojnacka-Wójcik E. Effects of a selective 5-HT1B receptor agonist and antagonists in animal models of anxiety and depression. Behavioural Pharmacology. 2004 Dec;15(8):523-34. PMID 15577451
  6. ^ Chojnacka-Wójcik E, Kłodzińska A, Tatarczyńska E. The anxiolytic-like effect of 5-HT1B receptor ligands in rats: a possible mechanism of action. Journal of Pharmacy and Pharmacology. 2005 Feb;57(2):253-7. PMID 15720791
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