Catalog Number: 1221
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
Biological Activity
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
  • M.Wt:
    557.09
  • Formula:
    C32H32N4O3.HCl
  • Solubility:
    Soluble to 10 mM in DMSO with gentle warming
  • Purity:
    >95%
  • Storage:
    Store at -20°C
  • CAS No:
    180084-26-8
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.
Additional Information
Licensing Caveats:
Sold with the permission of GlaxoSmithKline
Background References
  1. Stimulation of 5-HT1B receptors causes hypothermia in the guinea-pig.
    Hagan et al.
    Eur.J.Pharmacol., 1997;331:169
  2. 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
  3. 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
  4. SB-224289 - a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.
    Selkirk et al.
    Br.J.Pharmacol., 1998;125:202
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SB 224289 hydrochloride include:

5 Citations: Showing 1 - 5
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  1. Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells.
    Authors: Hirono
    Neuropharmacology 2017;118:79
  2. SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A.
    Authors: Cassilly Et al.
    Mol Ther 2016;11:e0154932
  3. Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres.
    Authors: Baillie Et al.
    PLoS One 2012;63:362
  4. Gene therapy by targeted adenovirus-mediated knockdown of pulmonary endothelial Tph1 attenuates hypoxia-induced pulmonary hypertension.
    Authors: Morecroft Et al.
    Neuron 2012;20:1516
  5. Serotonin reciprocally regulates melanocortin neurons to modulate food intake.
    Authors: Heisler Et al.
    J Neurosci 2006;51:239

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