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Submit ReviewJNJ 5207852 dihydrochloride
Description: High affinity H3 antagonist
Chemical Name: 1-[3-[4-(1-Piperidinylmethyl)phenoxy]propyl]piperidine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for JNJ 5207852 dihydrochloride
JNJ 5207852 dihydrochloride is a 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 for JNJ 5207852 dihydrochloride
| M. Wt | 389.4 |
| Formula | C20H32N2O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 1782228-76-5 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JNJ 5207852 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 19.47 | 50 | |
| DMSO | 7.79 | 20 with gentle warming |
Preparing Stock Solutions for JNJ 5207852 dihydrochloride
The following data is based on the product molecular weight 389.4. 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 |
|---|---|---|---|
| 0.5 mM | 5.14 mL | 25.68 mL | 51.36 mL |
| 2.5 mM | 1.03 mL | 5.14 mL | 10.27 mL |
| 5 mM | 0.51 mL | 2.57 mL | 5.14 mL |
| 25 mM | 0.1 mL | 0.51 mL | 1.03 mL |
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Product Datasheets for JNJ 5207852 dihydrochloride
References for JNJ 5207852 dihydrochloride
References are publications that support the biological activity of the product.
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 donep. 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
If you know of a relevant reference for JNJ 5207852 dihydrochloride, please let us know.
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Keywords: JNJ 5207852 dihydrochloride, JNJ 5207852 dihydrochloride supplier, JNJ5207852, histamine, receptor, H3, neutral, antagonist, antagonists, Histamine, Receptors, 4020, Tocris Bioscience
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Histamine Receptors Scientific Review
Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.
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