SB-216641

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]

SB-216641
Clinical data
ATC code
  • none
Identifiers
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
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC28H30N4O4
Molar mass486.572 g·mol−1
3D model (JSmol)
SMILES
  • CN(C)CCOc1cc(ccc1OC)NC(=O)c3ccc(cc3)-c2ccc(cc2C)-c4noc(C)n4
InChI
  • InChI=1S/C28H30N4O4/c1-18-16-22(27-29-19(2)36-31-27)10-12-24(18)20-6-8-21(9-7-20)28(33)30-23-11-13-25(34-5)26(17-23)35-15-14-32(3)4/h6-13,16-17H,14-15H2,1-5H3,(H,30,33)
  • Key:JRNUKVFYILMMLX-UHFFFAOYSA-N
  (verify)

References
  1. Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Göthert M, et al. (September 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. S2CID 26760453.
  2. Matsuoka T, Hasuo H, Akasu T (March 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. S2CID 35850798.
  3. Yan QS, Zheng SZ, Yan SE (September 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. S2CID 46700479.
  4. Lee JJ, Hahm ET, Lee CH, Cho YW (January 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 (December 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. S2CID 6940756.
  6. Chojnacka-Wójcik E, Kłodzińska A, Tatarczyńska E (February 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. S2CID 20743875.
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