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Submit ReviewGR 55562 dihydrochloride
Description: 5-HT1B antagonist
Chemical Name: 3-[3-(Dimethylamino)propyl]-4-hydroxy-N-[4-(4-pyridinyl)phenyl]benzamide dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for GR 55562 dihydrochloride
GR 55562 dihydrochloride is a selective competitive 5-HT1B (5-HT1Dβ) silent antagonist with pKB values of 7.3 and 6.3 for human cloned 5-HT1B and 5-HT1D receptors respectively and only weak binding at a number of other 5-HT subtypes.
Licensing Information
Sold with the permission of GlaxoSmithKline
Technical Data for GR 55562 dihydrochloride
| 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 Data for GR 55562 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 100 |
Preparing Stock Solutions for GR 55562 dihydrochloride
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 | 22.3 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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Product Datasheets for GR 55562 dihydrochloride
References for GR 55562 dihydrochloride
References are publications that support the biological activity of the product.
MacLean et al (1996) Evidence for 5-HT1-like receptor-mediated vasoconstriction in human pulmonary artery. Br.J.Pharmacol. 119 277 PMID: 8886409
Walsh et al (1995) The activity of 5-HT1D receptor ligands at cloned human 5-HT1Dα and 5-HT1Dβ receptors. Eur.J.Pharmacol. 287 79 PMID: 8666030
Connor et al (1995) Use of GR55562, a selective 5-HT1D antagonist, to investigate 5-HT1D receptor subtypes mediating cerebral vasoconstriction. Cephalalgia 15 99
If you know of a relevant reference for GR 55562 dihydrochloride, please let us know.
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Keywords: GR 55562 dihydrochloride, GR 55562 dihydrochloride supplier, 5-HT1B, antagonists, Serotonin, Receptors, GR55562, dihydrochloride, GlaxoSmithKline, GSK, 1054, Tocris Bioscience
9 Citations for GR 55562 dihydrochloride
Citations are publications that use Tocris products. Selected citations for GR 55562 dihydrochloride include:
Medrihan et al (2017) Initiation of Behavioral Response to Antidepressants by Cholecystokinin Neurons of the Dentate Gyrus. Neuron 95 564 PMID: 28735749
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
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
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
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
Johansson et al (2012) Expressional changes in cerebrovascular receptors after experimental transient forebrain ischemia. PLoS One 7 e41852 PMID: 22848635
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
Rataj et al (2018) Fingerprint-Based Machine Learning Approach to Identify Potent and Selective 5-HT2BR Ligands. Molecules 23 PMID: 29748476
McDaid and Docherty (2001) Vascular actions of MDMA involve alpha1 and alpha2-adrenoceptors in the anaesthetized rat. Br J Pharmacol 133 429 PMID: 11375260
Do you know of a great paper that uses GR 55562 dihydrochloride from Tocris? Please let us know.
Reviews for GR 55562 dihydrochloride
Average Rating: 5 (Based on 1 Review.)
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Antidepressantsby Cholecystokinin Neurons of the Dentate Gyrus.
By
Anonymous on 02/03/2020
Assay Type: In Vivo
Species: Mouse
100uM GR 55562
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