Biological Activity
Histamine H3 receptor antagonist (pKi values are 8.15 and 8.93 for rat and human H3 receptors respectively). Increases extracellular norepinephrine and acetylcholine levels in rat frontal cortex but does not stimulate dopamine release. Brain penetrant.
Licensing Information
Sold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
Technical Data
| M. Wt | 385.37 |
| Formula | C20H28N2O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 544707-20-2 |
| PubChem ID | 10237424 |
| InChI Key | PAQHERKZFLOHCA-UHFFFAOYSA-N |
| Smiles | C1(CN2CCOCC2)=CC=CC(C#CCCN3CCCCC3)=C1.Cl.Cl |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 9.63 | 25 | |
| water | 38.54 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 385.37. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.59 mL | 12.97 mL | 25.95 mL |
| 5 mM | 0.52 mL | 2.59 mL | 5.19 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.59 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bonaventure et al (2007) Histamine H3 receptor antagonists: from target identification to drug leads. Biochem.Pharmacol. 73 1084 PMID: 17129577
Esbenshade et al (2008) The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. Br.J.Pharmacol. 154 1166 PMID: 18469850
Boggs et al (2009) JNJ-10181457, a selective non-imidazole histamine H3 receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition. Neuropharmacology 56 1131 PMID: 19345233
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