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Updated: May 8, 2026

Assessment of Vascular Tone Responsiveness using Isolated Mesenteric Arteries with a Focus on Modulation by Perivascular Adipose Tissues
Published on: June 3, 2019
5-hydroxytryptamine and its receptors in systemic vascular walls
Takuji Machida1, Kenji Iizuka, Masahiko Hirafuji
1Department of Pharmacological Sciences, School of Pharmaceutical Sciences, Health Sciences University of Hokkaido.
Platelet-derived serotonin (5-HT) impacts vascular cells, influencing cardiovascular disease. 5-HT2A receptor antagonists like sarpogrelate show potential for novel cardiovascular therapies.
Area of Science:
- Cardiovascular Biology
- Pharmacology
- Cell Signaling
Background:
- Bloodstream serotonin (5-HT) is stored in platelets and affects vascular smooth muscle cells (VSMCs) and endothelial cells (ECs).
- 5-HT signaling through various receptors (e.g., 5-HT2A, 5-HT1, 5-HT4) influences VSMC proliferation, migration, and ECs' angiogenic potential.
- Dysregulated 5-HT activity contributes to cardiovascular pathophysiology.
Purpose of the Study:
- To elucidate the multifaceted roles of 5-HT receptors in vascular cell function and angiogenesis.
- To explore the therapeutic potential of 5-HT receptor antagonists, specifically sarpogrelate, in cardiovascular diseases.
Main Methods:
- Review of existing literature on 5-HT receptor signaling in VSMCs and ECs.
- Analysis of studies investigating the effects of 5-HT and its antagonists on cellular processes like proliferation, migration, and nitric oxide (NO) production.
- Examination of evidence linking 5-HT receptor activity to angiogenesis and vasodilator responses.
Main Results:
- 5-HT2A receptor activation in VSMCs promotes proliferation, migration, and alters NO and prostaglandin I2 production.
- 5-HT signaling via 5-HT1 and 5-HT4 receptors in ECs is crucial for angiogenesis.
- Sarpogrelate, a 5-HT2A antagonist, indirectly enhances 5-HT1B receptor function in ECs, potentially increasing NO production and vasodilation.
Conclusions:
- Understanding 5-HT receptor roles is key to developing new cardiovascular therapies.
- Existing drugs like sarpogrelate may have expanded clinical applications for cardiovascular conditions.
- Targeting 5-HT receptors offers a promising avenue for novel drug development in cardiovascular medicine.
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