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SB 224289 hydrochloride

Cat No. 1221

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Chemical Name: 1'-Methyl-5-[[2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3- yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo [2,3-f]indole-3,4'-piperidine hydrochloride

Biological Activity

Selective 5-HT_1B receptor antagonist (pK_i = 8.2). Displays > 60-fold selectivity over 5-HT_1D, 5-HT_1A, 5-HT_1E, 5-HT_1F, 5-HT_2A and 5-HT_2C receptors in radioligand binding and functional assays. Centrally active following oral administration in vivo.

Licensing Information

Sold with the permission of GlaxoSmithKline.

Technical Data

M.Wt:

557.09

Formula:

C₃₂H₃₂N₄O₃.HCl

Solubility:

Soluble to 10 mM in DMSO

Purity:

>98 %

Storage:

Store at RT

CAS No:

[180083-23-2]

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis and MSDS.

Resources

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch

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Material Safety Data Sheet: View current batch

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References

Hagan et al (1997) Stimulation of 5-HT_1B receptors causes hypothermia in the guinea-pig. Eur.J.Pharmacol. 331 169. Gaster et al (1998) The selective 5-HT_1B receptor inverse agonist 1¢-methyl-5-[[2¢-methyl-4¢-(5-methyl-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4¢-piperidine (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. J.Med.Chem. 41 1218. Roberts et al (1998) Differential effects of 5-HT_1B/1D receptor antagonists in dorsal and median raphe innervated brain regions. Eur.J.Pharmacol. 346 175. Selkirk et al (1998) SB-224289 - a novel selective (human) 5-HT_1B receptor antagonist with negative intrinsic activity. Br.J.Pharmacol. 125 202.

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Keywords: SB 224289 hydrochloride, Selective, 5-HT1B, antagonist, Serotonin, Receptors, SB224289, hydrochloride, GlaxoSmithKline, GSK

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