SB 224289 hydrochloride
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%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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Stimulation of 5-HT1B receptors causes hypothermia in the guinea-pig.
Hagan et al.
Eur.J.Pharmacol., 1997;331:169 -
SB-224289 - a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.
Selkirk et al.
Br.J.Pharmacol., 1998;125:202 -
Differential effects of 5-HT1B/1D receptor antagonists in dorsal and median raphe innervated brain regions.
Roberts et al.
Eur.J.Pharmacol., 1998;346:175 -
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
Gaster et al.
J.Med.Chem., 1998;41:1218
Product Datasheets
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Citations for SB 224289 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for SB 224289 hydrochloride include:
8 Citations: Showing 1 - 8
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Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells.
Authors: Hirono
Neuropharmacology 2017;118:79
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SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A.
Authors: Cassilly Et al.
Mol Ther 2016;11:e0154932
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Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres.
Authors: Baillie Et al.
PLoS One 2012;63:362
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Gene therapy by targeted adenovirus-mediated knockdown of pulmonary endothelial Tph1 attenuates hypoxia-induced pulmonary hypertension.
Authors: Morecroft Et al.
Neuron 2012;20:1516
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Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors.
Authors: Murray Et al.
J Neurophysiol 2011;106:925
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Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs.
Authors: Hampson Et al.
Diabetologia 2007;50:1743
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Serotonin reciprocally regulates melanocortin neurons to modulate food intake.
Authors: Heisler Et al.
J Neurosci 2006;51:239
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The role of serotonin (5-hydroxytryptamine1A and 1B) receptors in prostate cancer cell proliferation.
Authors: Siddiqui Et al.
J Urol 2006;176:1648
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