The Full Wiki

More info on SB-216,641

SB-216,641: Wikis


Note: Many of our articles have direct quotes from sources you can cite, within the Wikipedia article! This article doesn't yet, but we're working on it! See more info or our list of citable articles.


From Wikipedia, the free encyclopedia

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
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]


  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


Got something to say? Make a comment.
Your name
Your email address