SB 224289 hydrochloride

Cat. No. 1221

SB 224289 hydrochloride C32H32N4O3.HCl [180084-26-8]

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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-HT1B receptor antagonist (pKi = 8.2). Displays > 60-fold selectivity over 5-HT1D, 5-HT1A, 5-HT1E, 5-HT1F, 5-HT2A and 5-HT2C 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 with gentle warming
Purity:
>95 %
Storage:
Store at RT
CAS No:
180084-26-8

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

Gaster et al (1998) The selective 5-HT1B 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. PMID: 9548813.

Roberts et al (1998) Differential effects of 5-HT1B/1D receptor antagonists in dorsal and median raphe innervated brain regions. Eur.J.Pharmacol. 346 175. PMID: 9652357.

Selkirk et al (1998) SB-224289 - a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity. Br.J.Pharmacol. 125 202. PMID: 9776361.

Hagan et al (1997) Stimulation of 5-HT1B receptors causes hypothermia in the guinea-pig. Eur.J.Pharmacol. 331 169. PMID: 9274976.

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Keywords: SB 224289 hydrochloride, supplier, Selective, 5-HT1B, antagonist, Serotonin, Receptors, SB224289, hydrochloride, GlaxoSmithKline, GSK, Tocris Bioscience, 5-HT1B Receptor Antagonist products

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