Latrepirdine 2HCl

Catalog No.S1245

Latrepirdine 2HCl Chemical Structure

Molecular Weight(MW): 392.37

Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.

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Biological Activity

Description Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.
Targets
GluR [2] Histamine receptor [2] 5-HT [2]
In vitro

Latrepirdine increases succinate dehydrogenase activity (MTT-assay), mitochondrial membrane potential (DeltaPsim), and cellular ATP levels in primary mouse cortical neurons and human neuroblastoma cells (SH-SY5Y). Latrepirdine enhances mitochondrial function both in the absence and presence of stress and Dimebon-treated cells are partially protected to maintain cell viability. [1] Latrepirdine leads to enhanced mTOR- and Atg5-dependent autophagy in cultured mammalian cells. [2] latrepirdine stimulates MTOR- and ATG5-dependent autophagy, leading to the reduction of intracellular levels of APP metabolites, including Aβ in cultured cells. [3] Latrepirdine stimulates the degradation of α-syn in differentiated SH-SY5Y neurons, and in mouse brain following chronic administration, in parallel with elevation of the levels of markers of autophagic activity. [4] Latrepirdine increases intracellular ATP levels and glucose transporter 3 translocation to the plasma membrane in primary neuron. [5]

In vivo Latrepirdine treatment of TgCRND8 transgenic mice is associated with improved learning behavior and with a reduction in accumulation of Aβ42 and α-synuclein. [2] Latrepirdine administration results in increased levels of the biomarkers thought to correlate with autophagy activation in the brains of TgCRND8 (APP K670M, N671L, V717F) or wild-type mice, and that treatment is associated with abrogation of behavioral deficit, reduction in Aβ neuropathology, and prevention of autophagic failure among TgCRND8 mice. [3]

Protocol

Solubility (25°C)

In vitro DMSO 24 mg/mL (61.16 mM)
Ethanol 13 mg/mL (33.13 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 392.37
Formula

C21H25N3.2HCl

CAS No. 97657-92-6
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01085266 Terminated Huntington Disease Medivation, Inc.|Pfizer February 2010 Phase 3
NCT00954590 Terminated Moderate to Severe Alzheimer Medivation, Inc.|Pfizer October 2009 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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GluR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID