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ANG2002 - A Promising Neurotensin Derivative
Because neurotensin penetrates poorly through the blood-brain barrier (BBB), its potential as a therapeutic agent has been difficult to realize. However, ANG2002 is showing great potential as a first-in-class analgesic in preclinical studies.
Promising results with ANG2002 in five different pain models
ANG2002 is a new chemical entity formed by the conjugation of the peptide Angiopep-2 (ANG) and neurotensin. The analgesic effect of ANG2002 was demonstrated in five widely accepted preclinical models of acute pain, inflammatory pain, post-operative pain, and neuropathic pain. In all those models, the activity was equal or superior to morphine and gabapentin.
Brain uptake of ANG2002
The brain uptake was studied in vivo in mice and demonstrated that ANG2002 is transported very efficiently across the BBB. The transport rate is higher than that of unconjugated neurotensin. In vitro, ANG2002 is able to bind to the high affinity neurotensin receptor confirming that the derivative is retaining its activity compared to the native neurotensin.
Overall study results of ANG2002 are further validating the potential of the EPiC platform for the development of effective neurotherapeutics.
Data Presented at Neuroscience 2010
Data from preclinical studies of ANG2002 were presented at the 2010 American Society of Society for Neuroscience Annual Meeting in San Diego.
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