Cannabinoid Receptor Type 1 - Expression

Expression

The CB1 receptor is encoded by the gene CNR1, located on human chromosome 6. Two transcript variants encoding different isoforms have been described for this gene. CNR1 orthologs have been identified in most mammals.

The CB1 receptor is expressed pre-synaptically at both glutaminergic and GABAergic interneurons and effectively acts as a neuromodulator to inhibit release of glutamate and GABA. Repeated administration of receptor agonists may result in receptor internalization and/ or a reduction in receptor protein signalling.

The inverse agonist MK-9470 makes it possible to produce in vivo images of the distribution of CB1 receptors in the human brain with positron emission tomography.

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