Sigma-1 Receptor Specific Biological Functions, Protective Role, and Therapeutic Potential in Cardiovascular Diseases

Ahmed Almaamari1, Marwa Sultan1, Tao Zhang1

  • 1Department of Pharmacology, The Key Laboratory of Neural and Vascular Biology, Ministry of Education, The Key Laboratory of New Drug Pharmacology and Toxicology, Hebei Medical University, Shijiazhuang, 050017, Hebei, China.

Cardiovascular Toxicology
|February 12, 2025
PubMed

Insights

The sigma-1 receptor (S1R) shows promise in treating cardiovascular disease (CVD). Activating S1R may offer protective benefits, guiding future clinical trials for heart conditions.

Area of Science:

  • Cardiology
  • Pharmacology
  • Molecular Biology

Background:

  • Cardiovascular disease (CVD) is a major global health burden, necessitating novel therapeutic strategies.
  • The sigma-1 receptor (S1R) is implicated in cardiac pathophysiology, including hypertrophy, heart failure, and remodeling.

Purpose of the Study:

  • To review the mechanisms underlying S1R's role in cardiovascular disease.
  • To explore how S1R pathway modulation confers cardiovascular protection.
  • To inform the development of new CVD therapeutic agents targeting S1R.

Main Methods:

  • Literature review of preclinical and clinical studies on S1R and CVD.
  • Analysis of molecular pathways influenced by S1R activation in the cardiovascular system.

Main Results:

  • Preclinical evidence indicates S1R activation exerts beneficial cardiovascular effects.
  • S1R modulation influences key pathways involved in cardiac protection.

Conclusions:

  • S1R represents a promising therapeutic target for cardiovascular diseases.
  • Understanding S1R mechanisms can accelerate the development of effective CVD treatments.

Related Concept Videos

Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
2.3K
Adrenergic Antagonists: Pharmacological Actions of β-Receptor Blockers01:27

Adrenergic Antagonists: Pharmacological Actions of β-Receptor Blockers

β-receptor blockers significantly impact the cardiovascular system by counteracting catecholamine-induced sympathetic responses. These medications decrease heart rate, contractility, and cardiac output, potentially leading to cardiac depression, life-threatening bradycardia, and death. Therapeutically, β-blockers function as mild antihypertensives and are utilized in treating angina pectoris and cardiac arrhythmias. However, nonselective β-blockers inhibit β2-receptors in...
527
Adrenergic Receptors: ɑ Subtype01:31

Adrenergic Receptors: ɑ Subtype

Adrenoceptors are classified into α and ꞵ classes based on their potencies to catecholamine agonists. α-adrenoceptors show the following order of catecholamine potency:
Adrenaline ≥ Noradrenaline >> Isoprenaline
α-adrenoceptors are further divided into α1 and α2-adrenoceptors.
α1-Adrenoceptors: These receptors are located postsynaptically on the effector organs and cause constriction of smooth muscle mediated by activation of phospholipase...
1.4K
Blood Studies for Cardiovascular System II: CRP, Hcy, and Cardiac Natriuretic Peptide Markers01:19

Blood Studies for Cardiovascular System II: CRP, Hcy, and Cardiac Natriuretic Peptide Markers

Cardiac biomarkers are critical in diagnosing, prognosing, and managing cardiovascular diseases. Routine measurement of specific biomarkers such as B-type natriuretic peptide (BNP), C-reactive protein (CRP), and homocysteine (Hcy) is common practice in clinical settings to evaluate heart function and predict cardiovascular events.
These markers indicate stress or strain on the heart muscle:
Natriuretic Peptides (BNP)
Cardiac myocytes produce these hormones in response to ventricular stretching...
43
Regulation of the Cardiovascular System01:27

Regulation of the Cardiovascular System

The regulation of the cardiovascular system allows the body to adapt to various demands and maintain homeostasis.
The regulation of the cardiovascular system involves the autonomic nervous system (ANS), baroreceptors, and chemoreceptors, ensuring that heart rate and blood pressure are appropriately modulated in response to varying physiological demands.
The ANS comprises two main divisions: the sympathetic and parasympathetic nervous systems. The sympathetic nervous system enhances...
359
Internal Receptors01:31

Internal Receptors

Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
69.3K