Bavisant (dihydrochloride)

Modify Date: 2024-01-03 18:28:08

Bavisant (dihydrochloride) Structure
Bavisant (dihydrochloride) structure
Common Name Bavisant (dihydrochloride)
CAS Number 929622-09-3 Molecular Weight 402.35800
Density N/A Boiling Point N/A
Molecular Formula C19H29Cl2N3O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Bavisant (dihydrochloride)


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. IC50 Value: Target: H3 receptorin 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 1?mg/day, 3?mg/day and 10?mg/day groups, respectively; the change in the 10?mg/day group was not statistically superior to placebo (p=0.161), and hence statistical comparisons of the 1?mg/day and 3?mg/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

 Names

Name (4-cyclopropylpiperazin-1-yl)-[4-(morpholin-4-ylmethyl)phenyl]methanone,dihydrochloride
Synonym More Synonyms

 Bavisant (dihydrochloride) Biological Activity

Description 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. IC50 Value: Target: H3 receptorin 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 1?mg/day, 3?mg/day and 10?mg/day groups, respectively; the change in the 10?mg/day group was not statistically superior to placebo (p=0.161), and hence statistical comparisons of the 1?mg/day and 3?mg/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
Related Catalog
References

[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

[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.

 Chemical & Physical Properties

Molecular Formula C19H29Cl2N3O2
Molecular Weight 402.35800
Exact Mass 401.16400
PSA 36.02000
LogP 2.85670
Storage condition 2-8℃

 Synonyms

UNII-1B5560RN9F
Bavisant dihydrochloride
Bavisant dihydrochloride anhydrous
Bavisant (dihydrochloride)
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