Bavisant dihydrochloride

• CAT Number: I005528
• CAS Number: 929622-09-3
• Molecular Formula: C19H29Cl2N3O2
• Molecular Weight: 402.36
• Purity: ≥95%
• Synonyms: (4-cyclopropylpiperazin-1-yl)(4-(morpholinomethyl)phenyl)methanone dihydrochloride
• Target: Histamine Receptor
• Solubility: 10 mM in DMSO
• Storage: Store at -20°C

Bavisant Hcl (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.


in vitro: Bavisant completed a phase II ADHD trial, but no results have been reported [1]. 


in vivo: Mean change from baseline in the total ADHD-RS-IV score at day 42 (primary efficacy endpoint) was -8.8 in the placebo group versus -9.3, -11.2 and -12.2 in the bavisant 1mg/day, 3mg/day and 10mg/day groups, respectively; the change in the 10mg/day group was not statistically superior to placebo (p=0.161), and hence statistical comparisons of the 1mg/day and 3mg/day groups with placebo based on a step-down closed testing procedure were not performed [2]. 


Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2

Reference

[1]. Robert L. Hudkins, Rita Raddatz, Ming Tao, Discovery and Characterization of 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine H3 Receptor Inverse Agonist. J. Med. Chem. 2011, 54, 4781-4792 


[2]. Weisler RH, Pandina GJ, Daly EJ, Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs. 2012 May 1;26(5):421-34.