Cannabinoid receptor 1 (CB1R) (CB1R)

The Cannabinoid receptor 1 (CB1R) is a G protein-coupled receptor primarily expressed in the central nervous system, where it mediates the effects of endocannabinoids like anandamide and exogenous cannabinoids such as THC [1, 2]. It plays a fundamental role in regulating neurotransmitter release via retrograde signaling, influencing physiological processes including appetite, pain sensation, mood, and memory [4]. In the periphery, CB1R is involved in energy metabolism in the liver, adipose tissue, and gastrointestinal tract [2]. Dysregulation of CB1R signaling is associated with various conditions, including obesity, metabolic syndrome, chronic pain, and neurodegenerative disorders [4]. While CB1R is a significant therapeutic target, drugs like the inverse agonist rimonabant were withdrawn from the market due to severe psychiatric side effects, such as depression and suicidal ideation [3]. Current research focuses on peripheral CB1R antagonists and allosteric modulators to achieve therapeutic benefits while minimizing central nervous system toxicity [4]. Additionally, CB1R mRNA expression levels are often utilized as biomarkers to assess receptor density and activity in research and clinical studies [2].

Other names

CNR1CB1CB1RCannabinoid receptor 1 (brain)Central cannabinoid receptor

Agonism, Antagonism, Inverse agonism, Negative allosteric modulation