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
Biological ActivitySB 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.
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.
Stimulation of 5-HT1B receptors causes hypothermia in the guinea-pig.
Hagan et al.
SB-224289 - a novel selective (human) 5-HT1B receptor antagonist with negative intrinsic activity.
Selkirk et al.
Differential effects of 5-HT1B/1D receptor antagonists in dorsal and median raphe innervated brain regions.
Roberts et al.
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.
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
Monoaminergic modulation of GABAergic transmission onto cerebellar globular cells.
SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A.
Authors: Cassilly Et al.
Mol Ther 2016;11:e0154932
Sumatriptan inhibition of N-type calcium channel mediated signaling in dural CGRP terminal fibres.
Authors: Baillie Et al.
PLoS One 2012;63:362
Gene therapy by targeted adenovirus-mediated knockdown of pulmonary endothelial Tph1 attenuates hypoxia-induced pulmonary hypertension.
Authors: Morecroft Et al.
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
Stimulation of glycogen synthesis and inactivation of phosphorylase in hepatocytes by serotonergic mechanisms, and counter-regulation by atypical antipsychotic drugs.
Authors: Hampson Et al.
Serotonin reciprocally regulates melanocortin neurons to modulate food intake.
Authors: Heisler Et al.
J Neurosci 2006;51:239
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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