Bavisant dihydrochloride hydrate

Names

[ CAS No. ]:
1103522-80-0

[ Name ]:
Bavisant dihydrochloride hydrate

[Synonym ]:
Methanone,(4-cyclopropyl-1-piperazinyl)(4-(4-morpholinylmethyl)phenyl)-,hydrochloride,hydrate (1:2:1)
(4-Cyclopropylpiperazin-1-yl)(4-(morpholin-4-ylmethyl)phenyl)methanone dihydrochloride monohydrate
BAVISANT DIHYDROCHLORIDE
Bavisant dihydrochloride (USAN)
UNII-C1H7H5X3RE
Bavisant dihydrochloride hydrate
Bavisant (dihydrochloride hydrate)

Biological Activity

[Description]:

Bavisant Hcl hydrate(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]:

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor
Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor
Research Areas >> Neurological Disease

[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.


[Related Small Molecules]

Loratadine | Histamine | Pitolisant hydrochloride | Cimetidine | Osthole | Clemastine fumarate | Ebrotidine | JNJ-7777120 | Famotidine | Cetirizine Dihydrochloride | Desloratadine | Ketotifen fumarate | Lodoxamide | Meclizine dihydrochloride | Chlorpheniramine maleate

Chemical & Physical Properties

[ Molecular Formula ]:
C19H31Cl2N3O3

[ Molecular Weight ]:
420.37400

[ Exact Mass ]:
419.17400

[ PSA ]:
45.25000

[ LogP ]:
2.79240

[ Storage condition ]:
2-8℃

Related Compounds