BQ-123

BQ-123 is a synthetic peptide that acts as an endothelin receptor antagonist. It is primarily used in scientific research to study the role of endothelin-1, a potent vasoconstrictor, in various physiological and pathological processes.

Structure and Function

BQ-123 is a cyclic peptide composed of five amino acids. It is specifically designed to block the endothelin type A (ETA) receptor, one of the two main types of endothelin receptors found in the body. By blocking the ETA receptor, BQ-123 prevents endothelin-1 from exerting its vasoconstrictive effects, thereby promoting vasodilation and reducing blood pressure.

Applications in Research

BQ-123 has been widely used in biomedical research to investigate the role of endothelin-1 and the ETA receptor in various conditions, including hypertension, heart failure, pulmonary arterial hypertension, and cancer. It has also been used to study the potential therapeutic benefits of ETA receptor antagonism in these conditions.

Pharmacology

BQ-123 is typically administered intravenously in research settings. It has a high affinity for the ETA receptor and a much lower affinity for the endothelin type B (ETB) receptor. Its effects are therefore largely specific to the ETA receptor.

Safety and Side Effects

As a research tool, BQ-123 is not intended for use in humans outside of a controlled research setting. However, in animal studies, it has been generally well tolerated with few reported side effects.

See Also

• Endothelin-1
• Endothelin receptor
• Vasoconstriction
• Vasodilation