product name Latrepirdine
Description: Latrepirdine, also known as dimebolin, is an orally active, and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug. Latrepirdine has been shown to inhibit brain cell death in animal models of Alzheimers disease and Huntingtons disease. Research suggests it may also have cognition-enhancing effects in healthy individual. Latrepirdine has been used clinically in Russia and other countries, However, a Phase III clinical trial for Alzheimers disease treatment failed to show any benefit.
References: J Alzheimers Dis. 2010;21(2):389-402; Mol Psychiatry. 2013 Aug;18(8):889-97.
392.37
Formula
C21H25N3.2HCl
CAS No.
97657-92-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 24 mg/mL (61.2 mM)
Water: <1 mg/mL
Ethanol: 13 mg/mL (33.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19423174
| In Vitro |
In vitro activity: 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. Latrepirdine leads to enhanced mTOR- and Atg5-dependent autophagy in cultured mammalian cells. latrepirdine stimulates MTOR- and ATG5-dependent autophagy, leading to the reduction of intracellular levels of APP metabolites, including Aβ in cultured cells. 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. Latrepirdine increases intracellular ATP levels and glucose transporter 3 translocation to the plasma membrane in primary neuron. Kinase Assay: Cell Assay: |
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| 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. 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. |
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| Formulation & Dosage | |
| References | J Alzheimers Dis. 2010;21(2):389-402; Mol Psychiatry. 2013 Aug;18(8):889-97. |
