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:
  • Formula:
  • Solubility:
    Soluble to 10 mM in DMSO with gentle warming
  • Purity:
  • Storage:
    Store at RT
  • CAS No:
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

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

Showing Results 1 - 4 of 4

  1. SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A.
    Authors: Cassilly Et al.
    Mol Ther
  2. Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres.
    Authors: Baillie Et al.
    PLoS One
  3. Gene therapy by targeted adenovirus-mediated knockdown of pulmonary endothelial Tph1 attenuates hypoxia-induced pulmonary hypertension.
    Authors: Morecroft Et al.
  4. Serotonin reciprocally regulates melanocortin neurons to modulate food intake.
    Authors: Heisler Et al.
    J Neurosci
Tocris Bioscience is the leading supplier of novel and exclusive tools for life science research with over 30 years' experience in the industry. Tocris is a Bio-Techne brand.

Order Details


Contact Information

Molarity Calculator
Calculate the mass, volume or concentration required for a solution

The molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) x Volume (L) x Molecular Weight (g/mol)
An example of a molarity calculation using the molarity calculator:
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?

R&D Systems Guarantee

or select another batch:


Customer Information