SB 224289 hydrochloride

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Cat.No. 1221 - SB 224289 hydrochloride | C32H32N4O3.HCl | CAS No. 180084-26-8
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)
Datasheet
Citations (8)
Reviews (1)
Literature (4)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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

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


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Reviews for SB 224289 hydrochloride

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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

PMID: 27183222
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