Bavisant dihydrochloride hydrate

Short Summary : Human H3 receptor antagonist

Category : Neuroscience|Histamine Receptor

Purity : 0.98

CAS Number : 1103522-80-0

Formula : C19H31Cl2N3O3

Molecular Weight : 420.37

SMILE : C1CC1N2CCN(CC2)C(=O)C3=CC=C(C=C3)CN4CCOCC4.O.Cl.Cl

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : Bavisant dihydrochloride hydrate is a highly selective, orally active antagonist of the human H3 receptor [1]. The human H3 receptor is a G-protein coupled receptor, which is expressed in the central nervous system and to a lesser extent the peripheral nervous system. Histamine H3 receptors regulate the release of other neurotransmitters [1].Bavisant dihydrochloride hydrate is an 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 adults with ADHD, three dosages of bavisant (1 mg/day, 3 mg/day or 10mg/day) were evaluated. Compared with the placebo group (-8.8) in the total ADHD-RS-IV score at day 42 (primary efficacy endpoint), the scores were -9.3, -11.2 and -12.2 in the 1mg/day, 3mg/day and 10mg/day groups, respectively. The changes were not statistically superior to placebo. However, mean change from baseline was superior to placebo in the atomoxetine (-15.3) and OROS methylphenidate (-15.7) groups (p < 0.005). The two lower dosages showed a good tolerability profile [1].References:[1]. Weisler RH, Pandina GJ, Daly EJ, et al. Randomized clinical study of a histamine H3 receptor antagonist for the treatment of adults with attention-deficit hyperactivity disorder. CNS Drugs, 2012, 26(5): 421-434.

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