Bavisant

Modify Date: 2024-01-11 18:17:26

Bavisant structure	Common Name	Bavisant
	CAS Number	929622-08-2	Molecular Weight	329.43700
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₉H₂₇N₃O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Bavisant

Bavisant (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
Synonym	More Synonyms

Description	Bavisant (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, et al. 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.

Description

Related Catalog

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

References

[1]. Robert L, et al. 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.

Molecular Formula	C₁₉H₂₇N₃O₂
Molecular Weight	329.43700
Exact Mass	329.21000
PSA	36.02000
LogP	1.25270
Storage condition	2-8℃

morpholine

CAS#:110-91-8

4-[(4-Cycloprop...

CAS#:929622-21-9

~92%

Bavisant

CAS#:929622-08-2

Literature: Allison, Brett D.; Carruthers, Nicholas I.; Grice, Cheryl A.; Letavic, Michael A. Patent: US2007/66821 A1, 2007 ; Location in patent: Page/Page column 9 ; US 20070066821 A1

Precursor 1
CAS#:110-91-8 morpholine
DownStream 0

(4-cyclopropyl-piperazin-1-yl)-(4-morpholin-4-ylmethyl-phenyl)-methanone

UNII-9827P7LFVH

BAVISANT

Bavisant [USAN:INN]

Bavisant

Use of Bavisant

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Bavisant Biological Activity

Chemical & Physical Properties

Synthetic Route

Precursor & DownStream

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