LY451395 - CAS 375345-95-2
Catalog number: 375345-95-2
Category: Inhibitor
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Molecular Weight:
Incubation of LY451395 with Actinoplanes missouriensis NRRL B3342 generated several metabolites that were previously detected in the in vivo metabolism studies of the preclinical species. LY404187 and LY451395 reverses the central effects of an acutely intoxicating dose of ethanol in the rat. LY451395 significantly and dose-dependently reversed ethanol-induced deficits in both motor coordination and disruptions in an operant task where animals were trained to press a lever for food reward.
Mibampator; LY 451395; LY-451395
Canonical SMILES:
1.Multiple-dose plasma pharmacokinetic and safety study of LY450108 and LY451395 (AMPA receptor potentiators) and their concentration in cerebrospinal fluid in healthy human subjects.
Jhee SS1, Chappell AS, Zarotsky V, Moran SV, Rosenthal M, Kim E, Chalon S, Toublanc N, Brandt J, Coutant DE, Ereshefsky L. J Clin Pharmacol. 2006 Apr;46(4):424-32.
The objective of this study was to measure the steady-state cerebrospinal fluid (CSF) concentration of LY450108 and LY451395 (positive modulators of AMPA receptors) in healthy subjects after the administration of 1 mg and 5 mg. Secondary objectives included the evaluation of safety, pharmacokinetics, and steady-state ratio of plasma:CSF concentrations of LY450108 and LY451395 after multiple dosing. This study was an open-label, multiple oral dose study evaluating 1 mg and 5 mg LY450108 and 1 mg and 5 mg LY451395 in 12 (3 subjects per dosing group) healthy subjects, aged 18 to 49 years. Twelve healthy male subjects completed the study. LY450108 and LY451395 were quantifiable in CSF after 1-mg and 5-mg multiple-dose administrations with plasma:CSF ratio of 82:1 and 44:1, respectively. LY450108 and LY451395 1 mg and 5 mg were measured in the CSF. Single and multiple oral doses of LY450108 and LY451395 were determined to be safe and well tolerated in healthy subjects.
2.Mibampator (LY451395) randomized clinical trial for agitation/aggression in Alzheimer's disease.
Trzepacz PT1, Cummings J, Konechnik T, Forrester TD, Chang C, Dennehy EB, Willis BA, Shuler C, Tabas LB, Lyketsos C. Int Psychogeriatr. 2013 May;25(5):707-19. doi: 10.1017/S1041610212002141. Epub 2012 Dec 21.
BACKGROUND: Mibampator, an amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptor potentiator, was evaluated for treatment of agitation and aggression (A/A) in Alzheimer's disease (AD).
3.AMPA potentiator treatment of cognitive deficits in Alzheimer disease.
Chappell AS1, Gonzales C, Williams J, Witte MM, Mohs RC, Sperling R. Neurology. 2007 Mar 27;68(13):1008-12.
OBJECTIVE: To investigate the efficacy and safety of the positive alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid modulator LY451395 in patients with mild to moderate Alzheimer disease (AD) (Mini-Mental State Examination scores 14 to 26).
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CAS 375345-95-2 LY451395

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