SB-216641

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	170230-39-4  Y
PubChem CID	3292447
IUPHAR/BPS	28
ChemSpider	2541153
UNII	ZM4360761C
CompTox Dashboard (EPA)	DTXSID4043985
Chemical and physical data
Formula	C28H30N4O4
Molar mass	486.572 g·mol−1
3D model (JSmol)	Interactive image
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
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SB-216641 is a drug which is a selective antagonist for the serotonin receptor 5-HT_1B, with around 25x selectivity over the closely related 5-HT_1D receptor. ^[1] It is used in scientific research, ^{[2] [3] [4]} and has demonstrated anxiolytic effects in animal studies. ^{[5] [6]}

See also

• AR-A000002
• GR-55562
• GR-127935
• SB-236057

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.