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|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Gaster et al (1998) he 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
If you know of a relevant reference for SB 224289 hydrochloride, please let us know.
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Keywords: Selective 5-HT1B antagonist Serotonin Receptors SB224289 hydrochloride GlaxoSmithKline GSK 5-HT1B Receptors
5 Citations for SB 224289 hydrochloride
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
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
Heisler et al (2006) Serotonin reciprocally regulates melanocortin neurons to modulate food intake. J Neurosci 51 239 PMID: 16846858
Do you know of a great paper that uses SB 224289 hydrochloride from Tocris? If so please let us know.
Literature in this Area
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
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