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SB-224289 hydrochloride

Catalog No. T12841   CAS 180084-26-8
Synonyms: SB-224289A

SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.

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SB-224289 hydrochloride Chemical Structure
SB-224289 hydrochloride, CAS 180084-26-8
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1 mg In stock $ 34.00
5 mg In stock $ 80.00
10 mg In stock $ 128.00
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1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 98.09%
Purity: 97.82%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.
In vitro SB-224289 does not directly inhibit the PS synthase enzyme in this in vitro assay.SB-224289 has specific toxin-blocking ability and does not inhibit Cho1p. SB-224289 (100 μM-25 μM) shows consistent efficacy at producing Pap-A resistance. Moreover, SB-224289 specifically blocks the activity of papuamides and not other membrane disruptors. SB-224289 is unable to protect wild-type cells against KF, but it is able to provide protection against TPap-A[1]. SB-224289 has a pKi of 8 at human cloned 5-HT1B receptors and displays more than 80 fold selectivity over the closely related 5-HT1D receptor and a range of other receptors. SB-224289 is a potent antagonist(pEC50 of 7.9±0.1). SB-224289 evokes a parallel rightward shift in the 5-HT concentration response curve with pA2 of 8.4±0.2. SB-224289 (100 nM and 1 μM) also significantly increases [3H]-5HT release in electrically stimulated guinea-pig brain cortex slices[3].
In vivo SB 224289 is a potent antagonist with an ED50 of 3.6 mg/kg, p.o in SK&F-99101-induced hypothermia in the guinea-pig. SB 224289 (4 mg/kg, p.o) reverses sumatriptan-induced inhibition of 5-HT release showing that it is also a potent terminal 5-HT autoreceptor antagonist in vivo. SB 224289 (2-16 mg/kg, p.o) does not increase 5-HT levels in the fuinea-pig frontal cortex. However, SB 224289 (4 mg/kg, p.o) causes a significantly increase in levels of 5-HT in the fuinea-pig dentate gyrus[3].
Synonyms SB-224289A
Molecular Weight 557.08
Formula C32H33ClN4O3
CAS No. 180084-26-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 8.1mg/mL (14.5mM), ultrasonic and warming and heat to 60°C

TargetMolReferences and Literature

1. Cassilly CD, et al. SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A. PLoS One. 2016 May 16;11(5):e0154932. 2. Hoplight BJ, et al. The effects of SB 224289 on anxiety and cocaine-related behaviors in a novel object task. Physiol Behav. 2005 Apr 13;84(5):707-14. Epub 2005 Apr 13. 3. Gaster LM, et al. The selective 5-HT1B receptor inverse agonist SB-224289, potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. Ann N Y Acad Sci. 1998 Dec 15;861:270-1.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Anti-Cancer Compound Library Neurotransmitter Receptor Compound Library Bioactive Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library

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5-HT7 agonist 1 Donitriptan N-Desmethylclozapine Befiradol hydrochloride 2-Methyl-5-HT hydrochloride SB-269970 Methiothepin maleate Pardoprunox

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Keywords

SB-224289 hydrochloride 180084-26-8 GPCR/G Protein Neuroscience 5-HT Receptor SB 224289 Hydrochloride SB-224289 Hydrochloride SB-224289A SB224289 Hydrochloride inhibitor inhibit

 

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