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Abstract
Endocannabinoids activate two types of specific G-protein-coupled receptors (GPCRs), namely cannabinoid CB1 and CB2. Contrary to the psychotropic actions of agonists of CB1 receptors, and serious side effects of the selective antagonists of this receptor, drugs acting on CB2 receptors appear as promising drugs to combat CNS diseases (Parkinson's disease, Huntington's chorea, cerebellar ataxia, amyotrohic lateral sclerosis). Differential localization of CB2 receptors in neural cell types and upregulation in neuroinflammation are keys to understand the therapeutic potential in inter alia diseases that imply progressive neurodegeneration. Medicinal chemistry approaches are now engaged to develop imaging tools to map receptors in the living human brain, to develop more efficacious agonists, and to investigate the possibility to develop allosteric modulators.
Highlights
To date only two cannabinoid receptors have been identified and completely accepted as key members of the endocannabinoid signaling
CB2 receptor (CB2R)-mediated neuroprotection/neurorestoration mechanisms are of special interest in disorders that affect movement-related areas, such as (i) Parkinson’s and Huntington’s diseases, (ii) autosomal dominant spinocerebellar ataxias, and (iii) amyotrophic lateral sclerosis (ALS)
The aim of this article was to collect evidence generated in the last years in support of the therapeutic potential of compounds selectively targeting the CB2R
Summary
Gemma Navarro 1, 2, 3, Paula Morales 4, 5, Carmen Rodríguez-Cueto 2, 6, 7, Javier Fernández-Ruiz 2, 6, 7, Nadine Jagerovic 4 and Rafael Franco * 1, 2, 3. Specialty section: This article was submitted to Neurodegeneration, a section of the journal Frontiers in Neuroscience. Endocannabinoids activate two types of specific G-protein-coupled receptors (GPCRs), namely cannabinoid CB1 and CB2. Contrary to the psychotropic actions of agonists of CB1 receptors, and serious side effects of the selective antagonists of this receptor, drugs acting on CB2 receptors appear as promising drugs to combat CNS diseases (Parkinson’s disease, Huntington’s chorea, cerebellar ataxia, amyotrohic lateral sclerosis). Differential localization of CB2 receptors in neural cell types and upregulation in neuroinflammation are keys to understand the therapeutic potential in inter alia diseases that imply progressive neurodegeneration. Medicinal chemistry approaches are engaged to develop imaging tools to map receptors in the living human brain, to develop more efficacious agonists, and to investigate the possibility to develop allosteric modulators
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