SB 224289 hydrochloride
Cat. No. 1221
Chemical Name: 1'-Methyl-5-[[2'-methyl-4'-(5-methyl-1
Biological ActivitySelective 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 InformationSold with the permission of GlaxoSmithKline
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 / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
If you know of a relevant reference for SB 224289 hydrochloride please let us know.
Citations are publications that use Tocris products. Selected citations for SB 224289 hydrochloride include:
Hirono (2017) Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells. Neuropharmacology 118 79. PMID: 28300552.
Cassilly et al (2016) SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A. Mol Ther 11 e0154932. PMID: 27183222.
Baillie et al (2012) Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres. PLoS One 63 362. PMID: 22691374.
Morecroft et al (2012) Gene therapy by targeted adenovirus-mediated knockdown of pulmonary endothelial Tph1 attenuates hypoxia-induced pulmonary hypertension. Neuron 20 1516. PMID: 22525513.
Heisler et al (2006) Serotonin reciprocally regulates melanocortin neurons to modulate food intake. J Neurosci 51 239. PMID: 16846858.
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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