JNJ 5207852 dihydrochloride
Cat. No. 4020
Chemical Name: 1-[3-[4-(1-Piperidinylmethyl)phenox
Biological ActivityHigh 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 InformationSold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
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.
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.
Barbier et al (2004) Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist. Br.J.Pharmacol. 143 649. PMID: 15466448.
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