GR 55562 dihydrochloride

Name: GR 55562 dihydrochloride
Brand: Tocris Bioscience
SKU: 1054
Rating: 5 (1 reviews)

Catalog # 1054

Citations (9)

(1)

COA / SDS

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Key Product Details

Description:	5-HT_1B antagonist
Chemical Name:	3-[3-(Dimethylamino)propyl]-4-hydroxy-N-[4-(4-pyridinyl)phenyl]benzamide dihydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	448.39

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Biological Activity

GR 55562 dihydrochloride is a selective competitive 5-HT_1B (5-HT_1Dβ) silent antagonist with pK_B values of 7.3 and 6.3 for human cloned 5-HT_1B and 5-HT_1D receptors respectively and only weak binding at a number of other 5-HT subtypes.

Licensing Information

Sold with the permission of GlaxoSmithKline

Technical Data

M. Wt	448.39
Formula	C₂₃H₂₅N₃O₂.2HCl
Storage	Desiccate at +4°C
Purity	≥98% (HPLC)
CAS Number	159533-25-2
PubChem ID	56972159
InChi Key	KBKWJHYQFQONBJ-UHFFFAOYSA-N
Smiles	Cl.Cl.CN(C)CCCC1=CC(=CC=C1O)C(=O)NC1=CC=C(C=C1)C1=CC=NC=C1

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.

Solubility

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water		100

Preparing Stock Solutions

The following data is based on the product molecular weight 448.39.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.23 mL	11.15 mL	22.30 mL
5 mM	0.45 mL	2.23 mL	4.46 mL
10 mM	0.22 mL	1.12 mL	2.23 mL
50 mM	0.04 mL	0.22 mL	0.45 mL

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References

References are publications that support the biological activity of the product.

MacLean Evidence for 5-HT₁-like receptor-mediated vasoconstriction in human pulmonary artery. Br.J.Pharmacol. 1996 PMID: 8886409
Walsh The activity of 5-HT_1D receptor ligands at cloned human 5-HT_1Dα and 5-HT_1Dβ receptors. Eur.J.Pharmacol. 1995 PMID: 8666030
Connor Use of GR55562, a selective 5-HT_1D antagonist, to investigate 5-HT_1D receptor subtypes mediating cerebral vasoconstriction. Cephalalgia

Citations for GR 55562 dihydrochloride (9)

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Citations are publications that use Bio-Techne products. Selected citations for GR 55562 dihydrochloride include:

Zhou et al. (2019) Modulation of Kalirin-7 Expression by Hippocampal CA1 5-HT1B Receptors in Spatial Memory Consolidation. Behav Brain Res. 356:148
PMID: 29949735
Rataj et al. (2018) Fingerprint-Based Machine Learning Approach to Identify Potent and Selective 5-HT2BR Ligands. Molecules. 23
PMID: 29748476
Medrihan et al. (2017) Initiation of Behavioral Response to Antidepressants by Cholecystokinin Neurons of the Dentate Gyrus. Neuron. 95:564
PMID: 28735749
Johansson et al. (2012) Expressional changes in cerebrovascular receptors after experimental transient forebrain ischemia. PLoS One. 7:e41852
PMID: 22848635
Wei et al. (2010) JNK regulates serotonin-mediated proliferation and migration of pulmonary artery smooth muscle cells. Am J Physiol Lung Cell Mol Physiol. 298:L863
PMID: 20228179
Morecroft et al. (2010) In vivo effects of a combined 5-HT1B receptor/SERT antagonist in experimental pulmonary hypertension. Exp Eye Res. 85:593
PMID: 19736308
Guo and Rainnie (2010) Presynaptic 5-HT(1B) receptor-mediated serotonergic inhibition of glutamate transmission in the bed nucleus of the stria terminalis. Neuroscience. 165:1390
PMID: 19963045
Müller et al. (2009) 5-hydroxytryptamine modulates migration, cytokine and chemokine release and T-cell priming capacity of dendritic cells in vitro and in vivo. PLoS One. 4:e6453
PMID: 19649285
McDaid and Docherty (2001) Vascular actions of MDMA involve alpha1 and alpha2-adrenoceptors in the anaesthetized rat. Br J Pharmacol. 133:429
PMID: 11375260

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Antidepressantsby Cholecystokinin Neurons of the Dentate Gyrus

Name: Anonymous

Species: Mouse

Assay Type: In Vivo

100uM GR 55562

PMID: 28735749

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