An SSRI; inhibits depletion of 5-HT induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex

Alaproclate (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
60719-83-7
Storage:
-20
UN-No:
Non-Hazardous - /

Alaproclate is a selective serotonin reuptake inhibitor (SSRI).{27770,45384} It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively).{27770} Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.{45384} It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer’s disease when administered at a dose of 20 mg/kg twice daily.{35772} Alaproclate (40 mg/kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.{45385}  

 

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Description

An SSRI; inhibits depletion of 5-HT induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg/kg, respectively); inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively); increases SIRT1 levels in N2a murine neuroblastoma cells expressing ApoE4 (IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer’s disease at 20 mg/kg twice daily; decreases immobility time in the forced swim test in rats at 40 mg/kg

Formal name: alanine, 2-(4-chlorophenyl)-1,1-dimethylethyl ester, monohydrochloride

Synonyms:  A03|GEA 654

Molecular weight: 292.2

CAS: 60719-83-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Depression||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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