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Data published confirming sigma-1 receptor’s beneficial direct interaction with cannabinoid receptor

Anavex Life Sciences Corp. welcomes new data published in the current issue of the International Journal of Neuropsychopharmacology (IJNP) revealing that the sigma-1 receptor, the Company’s drug target, interacts positively and directly with the . The current scientific findings indicate that sigma-1 receptor modulation may protect against psychosis possibly connected to cannabis (marijuana) abuse, especially among the young, whose nervous systems are still maturing, or individuals with a genetic predisposition, which could potentially lead to schizophrenia.

Given the potential therapeutic benefit of cannabis as well as the increased use of in the general population, these findings highlight the need for a stronger scientific understanding of cannabis or its components in indications such as and neurological diseases. Understanding cannabinoid receptor modulation will help reduce the potentially negative influence of cannabis. It will also assist with the development of drugs to treat psychosis possibly caused by cannabis.

The data published in IJNP indicates that the sigma-1 receptor acts as a stability system for the interaction of the cannabinoid receptor 1 (CB1) and the glutamate N-methyl-D-aspartate (NMDA) receptor. The calcium-sensitive sigma-1 receptor appears to function as a safety switch, releasing (NMDAR) from the influence of and avoiding glutamate hypofunction, a condition commonly found in schizophrenia.

“This study could encourage the exploration of marijuana components in combination with sigma-1 receptor drug candidates in order to understand the potential therapeutic benefit for neurodegenerative diseases, including Alzheimer’s, schizophrenia and neuropathic pain,” said Dr. Chuanhai Cao, Assistant Professor at the University of South Florida (USF) Health Byrd Alzheimer’s Institute. Dr. Cao and colleagues recently published a report showing that a compound in marijuana has potential applications in Alzheimer’s treatment.

“With Anavex drug candidates targeting the sigma-1 receptor, and with the mechanism of action being further validated, we are even more encouraged to advance our studies with additional neurodegenerative diseases,” said Christopher U. Missling, PhD, President and Chief Executive Officer of Anavex. “The Company is intrigued to realize the direct link to the body’s endocannabinoid system and to proceed with potential studies with our sigma-1 drugs candidates and cannabinoids.”

“Our work with the sigma-1 receptor has uncovered relevant aspects of its function in the neuronal plasma membrane as regulator of G protein-coupled receptor (GPCR)-NMDAR cross-regulation. From this point, our research can advance into neuropathic pain, mental illnesses and also certain neurodegenerative diseases in which their genesis or progression requires an altered NMDAR function,” said Dr. Javier Garzon, lead researcher of the paper.

The report, entitled “The calcium-sensitive Sigma-1 receptor prevents cannabinoids from provoking glutamate hypofunction: implications in antinociception and psychotic diseases,” was authored by Dr. Javier Garzon and colleagues from Neuropharmacology, Cajal Institute, CSIC in Madrid, Spain and Drug Discovery and Preclinical Development, Esteve, Barcelona, Spain.


The calcium-sensitive Sigma-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases, Pilar Sánchez-Blázquez, María Rodríguez-Muñoz, Raquel Herrero-Labrador, Javier Burgueño, Daniel Zamanillo and Javier Garzón, International Journal of Neuropsychopharmacology, DOI: 10.1017/S1461145714000029, originally published online 31 January 2014.

Source: Anavex Life Sciences Corp.