关键词: agonists antagonists biased signaling mental disorders serotonin receptor 2

Mesh : Animals Drug Design Humans Obesity / drug therapy physiopathology Patents as Topic Receptors, Serotonin, 5-HT2 / drug effects metabolism Schizophrenia / drug therapy physiopathology Serotonin / metabolism Serotonin 5-HT2 Receptor Agonists / pharmacology therapeutic use Serotonin 5-HT2 Receptor Antagonists / pharmacology therapeutic use Substance-Related Disorders / drug therapy physiopathology

来  源:   DOI:10.1517/13543776.2016.1113257   PDF(Sci-hub)

Abstract:
BACKGROUND: Serotonin or 5-hydroxytryptamine (5-HT) is a substance found in plasma, which increases smooth muscle contraction and mediates platelet aggregation. In addition, it is a monoamine neurotransmitter and is implicated in diverse behaviors. The serotonin receptor 2 (5-HT2) subfamily is best known for biased signaling and is strongly expressed mainly in the brain regions postulated to be involved in the modulation of higher cognitive and affective functions. Modulators of the 5-HT2 receptor are currently used to treat a variety of diseases including chronic pain and psychonosema. These properties suggest that 5-HT2 receptors may become an important therapeutic target for the treatment of various pathological conditions.
METHODS: This review highlights the significant progress that has been made in the discovery and development of 5-HT2 receptor agonists and antagonists based on an analysis of the patent literature between January 2004 and December 2014.
CONCLUSIONS: Cumulative evidence over the past decade supports the notion that the modulation of 5-HT2 receptors has a positive effect on human cognition and emotion. Therefore, we suggest that new agonists and antagonists may play an important role in the treatment of disorders such as schizophrenia, addiction and obesity.
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