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Neuroprotective Compounds to Treat ParkinsonΓÇÖs Disease

技术优势

- Orally bioavailable- Crosses the blood-brain barrier- Efficacy data in 3 animal models for ParkinsonΓÇÖs Disease- Accumulates in the substantia nigra and striatum within 1 hour, and persists for at least 24 hours- Protects dopaminergic neurons in vivo- Improved motor coordination (pole test, Rotor-Rod) and hyposmia (scent test)- No apparent long-term (12 months) side-effects or toxicity at therapeutically effective doses in a mouse model for PDIssued patents with broad composition of matter claims for Mito-apocynins and multiple derivative compounds, and method claims to:- Increase dopamine or dopac in the brain- Prevent a decrease in brain dopamine levels in Parkinson's disease- Reduce brain inflammation and/or neurotransmitter deficits- Delay neurodegeneration or lessen the effect of disease symptoms- Prolong motor function in a mammal with a neurodegenerative disease

详细技术说明

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*Abstract

Mito-apocynins are novel, mitochondria-targeting apocynin derivatives that prevent the development of ParkinsonΓÇÖs disease (PD)-like symptoms such as loss of coordinated motor function and hyposmia (deficits in sense of smell) in mouse models for PD.Apocynin is a naturally-occurring molecule previously shown to protect dopaminergic neuronal cells in an MPTP model of PD. Mito-apocynins are apocynin linked to a mitochondria-targeting triphenylphosphonium cation moiety (TPP+) via carbon chain linkers, thus enhancing cell-permeability and enabling selective targeting to mitochondria. Mito-apocynins are 60 to 100-fold more potent in vivo than other neuroprotective forms of apocynin (e.g., diapocynin), exerting significant neuroprotective effects with no apparent toxicity when administered orally (3 mg/kg), 3 times per week for up to 12 months.

*Principal Investigation

Name: Balaraman Kalyanaraman

Department:

国家/地区

美国