Date: 2015-02-19
Type of information: Presentation of results at a congress
phase: preclinical
Announcement: presentation of results at the 2014 American Neuroscience Meeting, Washington D.C.
Company: Addex Therapeutics (Switzerland)
Product: ADX92639
Action
mechanism: ADX92639 is a negative allosteric modulator of metabotropic glutamate receptor subtype. The metabotropic receptor 2 (mGluR2) belongs to the class C GPCR family (group II mGluRs). This receptor shows a broad distribution throughout the cortex as well as high expression in the hippocampus and perforant path. Activation of mGluR2 leads to inhibition of glutamate release in the synapse and mGluR2 NAM is one of the most promising experimental therapeutic strategies for the treatment of cognitive impairment in Alzheimer\'s disease.
Disease:
Therapeutic area: Neurodegenerative diseases - Neurological diseases
Country:
Trial details:
Latest
news: * On February 19, 2015, Addex Therapeutics, a company pioneering allosteric modulation-based drug discovery and development announced that systemic treatment with its proprietary mGlu2 receptor negative allosteric modulator (NAM), ADX92639, protects vulnerable neurons against global ischemia in rats. The neuroprotective effect of ADX92639 was studied in the 4-vessel occlusion (4VO) model of transient global ischemia in adult male rats. 4VO causes extensive degeneration of hippocampal CA1 pyramidal neurons, whereas neurons of the CA3 region are relatively spared. ADX92639 protected the CA1 neurons from ischemic neuronal death after oral administration of 30 mg/kg. The study builds on the evidence that induction of ischemia causes changes in the expression of mGlu2 receptors in the vulnerable CA1 region of the hippocampus. The data presented at the 2014 American Neuroscience Meeting, Washington D.C., was generated in collaboration with Marta Motolese, Federica Mastroiacovo, Milena Cannella, Giuseppe Battaglia and Ferdinando Nicoletti of IRCCS Neuromed, Italy.
