Biological Activity
High affinity histamine H3 receptor neutral antagonist (pKi values are 8.9 and 9.2 in rat and human respectively). Brain penetrant and orally active. Has 3- and 100-fold higher affinity than thioperamide (Cat. No. 0644) for rat and human H3 receptors respectively. Suppresses slow-wave sleep; exhibits wake-promoting effects in rodent arousal models.
Licensing Information
Sold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
Technical Data
M. Wt | 389.4 |
Formula | C20H32N2O.2HCl |
Storage | Desiccate at RT |
Purity | ≥99% (HPLC) |
CAS Number | 398473-34-2 |
PubChem ID | 90488903 |
InChI Key | RLLXSVVZCGBIJR-UHFFFAOYSA-N |
Smiles | C1(CN2CCCCC2)=CC=C(OCCCN3CCCCC3)C=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 | |||
DMSO | 7.79 | 20mM with gentle warming | |
water | 19.47 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 389.4. 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 | 2.57 mL | 12.84 mL | 25.68 mL |
5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
10 mM | 0.26 mL | 1.28 mL | 2.57 mL |
50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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References
References are publications that support the products' biological activity.
Barbier et al (2004) Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br.J.Pharmacol. 143 649 PMID: 15466448
Jia et al (2005) Effects of histamine H3 antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in weanling mice. Neuropharmacology 50 404 PMID: 16310812
Le et al (2008) Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists. J.Pharmacol.Exp.Ther. 325 902 PMID: 18305012
Keywords: JNJ 5207852 dihydrochloride, supplier, JNJ5207852, histamine, receptor, H3, neutral, antagonist, antagonists, Histamine, H3, Receptors, Histamine, H3, Receptors, Tocris Bioscience