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Submit ReviewSB 224289 hydrochloride
Description: Selective 5-HT1B antagonist
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
Purity: ≥95% (HPLC)
Biological Activity for SB 224289 hydrochloride
SB 224289 hydrochloride is a 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 for SB 224289 hydrochloride
| M. Wt | 557.09 |
| Formula | C32H32N4O3.HCl |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 180084-26-8 |
| PubChem ID | 11226716 |
| InChI Key | GKGKBZYMDILCOF-UHFFFAOYSA-N |
| Smiles | O=C(C5=CC=C(C6=CC=C(C7=NOC(C)=N7)C=C6C)C=C5)N2C1=CC3=C(OCC43CCN(CC4)C)C=C1CC2.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SB 224289 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 5.57 | 10 with gentle warming |
Preparing Stock Solutions for SB 224289 hydrochloride
The following data is based on the product molecular weight 557.09. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 17.95 mL | 89.75 mL | 179.5 mL |
| 0.5 mM | 3.59 mL | 17.95 mL | 35.9 mL |
| 1 mM | 1.8 mL | 8.98 mL | 17.95 mL |
| 5 mM | 0.36 mL | 1.8 mL | 3.59 mL |
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Product Datasheets for SB 224289 hydrochloride
References for SB 224289 hydrochloride
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for SB 224289 hydrochloride, please let us know.
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Keywords: SB 224289 hydrochloride, SB 224289 hydrochloride supplier, Selective, 5-HT1B, antagonist, Serotonin, Receptors, SB224289, hydrochloride, GlaxoSmithKline, GSK, 1221, Tocris Bioscience
8 Citations for SB 224289 hydrochloride
Citations are publications that use Tocris products. Selected citations for SB 224289 hydrochloride include:
Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728
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
Siddiqui et al (2006) The role of serotonin (5-hydroxytryptamine1A and 1B) receptors in prostate cancer cell proliferation. J Urol 176 1648 PMID: 16952708
Heisler et al (2006) Serotonin reciprocally regulates melanocortin neurons to modulate food intake. J Neurosci 51 239 PMID: 16846858
Hampson et al (2007) Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs. Diabetologia 50 1743 PMID: 17579833
Do you know of a great paper that uses SB 224289 hydrochloride from Tocris? Please let us know.
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The 5,760 bioactive compound library is a collated compound set of approved drugs and biologically active compound.
By
Anonymous on 02/01/2020
Assay Type: In Vitro
Species: Other
Biologically active compounds that have been documented to interact with awide range of targets including SB-224289 (Cat. # 1221), MG-624 (Cat.# 1356), GVIA (Cat. No. 1085), DPAT hydrobromide (Cat. No. 1080) and valinomycin (VA; Cat. # 3373) were ordered from Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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