1103522-80-0

1103522-80-0 structure
1103522-80-0 structure
  • Name: Bavisant dihydrochloride hydrate
  • Chemical Name: (4-cyclopropylpiperazin-1-yl)-[4-(morpholin-4-ylmethyl)phenyl]methanone,hydrate,dihydrochloride
  • CAS Number: 1103522-80-0
  • Molecular Formula: C19H31Cl2N3O3
  • Molecular Weight: 420.37400
  • Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
  • Create Date: 2017-01-15 23:02:49
  • Modify Date: 2024-01-01 20:41:29
  • 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

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

Molecular Formula C19H31Cl2N3O3
Molecular Weight 420.37400
Exact Mass 419.17400
PSA 45.25000
LogP 2.79240
Storage condition 2-8℃