Author:

Keywords:

positron-emission-tomography, endocannabinoid system, multiple-sclerosis, selective antagonist, inverse agonist, rat-brain, pet radioligand, f-18 sr144385, primate brain, binding, Science & Technology, Life Sciences & Biomedicine, Pharmacology & Pharmacy, POSITRON-EMISSION-TOMOGRAPHY, ENDOCANNABINOID SYSTEM, MULTIPLE-SCLEROSIS, SELECTIVE ANTAGONIST, INVERSE AGONIST, RAT-BRAIN, PET RADIOLIGAND, F-18 SR144385, PRIMATE BRAIN, BINDING, Brain, Drug Design, Humans, Ligands, Molecular Structure, Positron-Emission Tomography, Protein Binding, Radioligand Assay, Radiopharmaceuticals, Receptor, Cannabinoid, CB1, 1115 Pharmacology and Pharmaceutical Sciences, Medicinal & Biomolecular Chemistry, 3214 Pharmacology and pharmaceutical sciences

Abstract:

Cerebral cannabinoid receptor (CB1) and cannabinoid drugs constitute a vibrant field in modern medicine and pharmacology. However, the physiological and pharmacological roles played by the cannabinoid receptor in the central nervous system are still not fully understood. Positron-emission tomography (PET) is the most advanced technique for non-invasive research of cerebral receptors. Quantitative PET imaging of CB1 in animal and human brains has been limited by drawbacks of the available CB1 radioligands that manifested low specific binding, high non-specific binding and/or low brain uptake.