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Updated: Feb 13, 2026

In Silico Clinical Trials for Cardiovascular Disease
Published on: May 27, 2022
Calcium sensing receptor expression and signalling in cardiovascular physiology and disease
Rolf Schreckenberg1, Klaus-Dieter Schlüter1
1Justus-Liebig-Universität Gießen, Physiologisches Institut, Germany.
Insights
The calcium sensing receptor (CaSR) plays vital roles in cardiovascular tissues, influencing vascular function and cardiac health. While CaSR antagonism shows promise for pulmonary hypertension, broad therapeutic use remains distant due to complex cell-specific effects.
Area of Science:
- Cardiovascular Biology
- Receptor Physiology
- Pharmacology
Background:
- The calcium sensing receptor (CaSR) is ubiquitously expressed, with significant roles beyond the parathyroidea.
- CaSR is present in various cardiovascular cell types, including endothelial cells, smooth muscle cells, cardiac fibroblasts, and myocytes.
Purpose of the Study:
- To review the physiological and pathological roles of CaSR in vascular and cardiac tissues.
- To explore the potential therapeutic implications of modulating CaSR activity in cardiovascular diseases.
Main Methods:
- Literature review focusing on CaSR expression and function in cardiovascular research.
- Analysis of studies investigating CaSR's involvement in vascular regulation, cell proliferation, and cardiac function.
Main Results:
- Endothelial CaSR regulates local perfusion via nitric oxide release; smooth muscle CaSR influences proliferation.
- CaSR contributes to pulmonary hypertension, suggesting antagonism as a therapeutic strategy.
- Cardiac CaSR impacts extracellular matrix composition and may mediate protective effects of ischemic pre-conditioning.
Conclusions:
- CaSR is a key regulator in cardiovascular physiology, affecting both vascular and cardiac systems.
- Despite its roles, the complex, cell-specific actions of CaSR currently limit its direct therapeutic application as activators or inhibitors.
Abstract:
Initially identified in the parathyroidea, the calcium sensing receptor (CaSR) is now recognized as an ubiquitously expressed receptor that exerts specific functions in multiple organs including the cardiovascular system. This review will focus on the role that CaSR plays in vascular and cardiac tissues. In the vasculature, CaSR is expressed in endothelial and smooth muscle cells. CaSR of endothelial cells participates in part to the regulation of local perfusion by linkage of CaSR activation to endothelial hyperpolarization and nitric oxide release. CaSR of smooth muscle cells is involved in the control of proliferation. In the pulmonary vasculature, however, CaSR participates in the onset of pulmonary hypertension, making CaSR antagonism a therapeutic option in this case. In the heart, CaSR is expressed in cardiac fibroblasts and myoyctes, contributing to normal cardiac function and composition of extracellular matrix. More important, activation of CaSR may participate in the cardiac protective effects of ischaemic pre-conditioning. In conclusion, CaSR plays an important physiological role in many regulatory pathways of the cardiovascular system, but due to the complex interaction between various cardiovascular cells and cell-specific effects, use of activators or inhibitors of CaSR for treatment of specific disease forms is yet not on the way.
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