SB 224289 hydrochloride
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.
Sold with the permission of GlaxoSmithKline
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||5.57||10mM with gentle warming|
Preparing Stock Solutions
The following data is based on the product molecular weight 557.09. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.8 mL||8.98 mL||17.95 mL|
|5 mM||0.36 mL||1.8 mL||3.59 mL|
|10 mM||0.18 mL||0.9 mL||1.8 mL|
|50 mM||0.04 mL||0.18 mL||0.36 mL|
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 J.Med.Chem. 41 1218 PMID: 9548813
Hagan et al (1997) Stimulation of 5-HT1B receptors causes hypothermia in the guinea-pig. Eur.J.Pharmacol. 331 169 PMID: 9274976
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
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Keywords: SB 224289 hydrochloride, supplier, Selective, 5-HT1B, antagonist, Serotonin, Receptors, SB224289, hydrochloride, GlaxoSmithKline, GSK, 5-HT1B, Receptors, 5-HT1B, Receptors, Tocris Bioscience
5 Citations for SB 224289 hydrochloride
Citations are publications that use Tocris products. Selected citations for SB 224289 hydrochloride include:
Heisler et al (2006) Serotonin reciprocally regulates melanocortin neurons to modulate food intake. J Neurosci 51 239 PMID: 16846858
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
Baillie et al (2012) Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres. PLoS One 63 362 PMID: 22691374
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
Do you know of a great paper that uses SB 224289 hydrochloride from Tocris? If so please let us know.
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