摘要：

The Cannabinoid 1 receptor (CB1) is a type A G-protein coupled receptor (GPCR) expressed most widely in the human brain and has been identified as a key receptor in modulating a number of physiological functions of the human body. Therefore, drugs acting on the CB1 have an enormous pharmacotherapeutic potential in disease conditions such as chronic neuropathic pain, cardio-metabolic diseases, obesity, and even in neurodegenerative diseases such as Alzheimer's disease and Parkinson's disease. In order to develop CB1-specific, high-affinity ligands, a better understanding of the structural aspects of the receptor in its native state is essential. Using an based cell-free () expression system in addition with nanolipid bilayers (Nanodiscs), we developed a convenient method for efficient production of the re-engineered human cannabinoid receptor and showed proof of functionality of the expressed receptor using a radioligand-binding assay. The saturation binding curve with CP55,940, a non-classical bicyclic analog of Δ -tetrahydrocannabinol (Δ-THC), showed Bof 1358 pmoles/g and a Kof 8.57 nM. The total amount of functional receptor was calculated to be 500 ng/ml of expression reaction.

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