JNJ 5207852 dihydrochloride

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Cat.No. 4020 - JNJ 5207852 dihydrochloride | C20H32N2O.2HCl | CAS No. 398473-34-2
Description: High affinity H3 receptor antagonist
Chemical Name: 1-[3-[4-(1-Piperidinylmethyl)phenoxy]propyl]piperidine hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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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Product Datasheets

Safety Datasheet

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


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