BQ-788
Also known as: BQ788, ETB receptor antagonist BQ-788, N-cis-2,6-dimethylpiperidinocarbonyl-L-gamma-methylleucyl-D-1-methoxycarbonyltryptophanyl-D-norleucine
Summary
BQ-788 is a synthetic peptide-based selective endothelin B (ET-B) receptor antagonist used primarily as a pharmacological research tool. It has been employed in experimental studies to dissect the roles of ET-A vs ET-B receptors in cardiovascular regulation, vascular tone, tumor biology, and pain signaling. It is not approved for clinical use.
Mechanism of Action
Selective competitive antagonist of the endothelin B (ET-B) receptor, blocking the vasoconstrictive and proliferative effects of endothelin-1 mediated through ET-B receptors.
Routes of Administration
Goals & Uses
- Pain and nociception researchNeuroscience ResearchLow
- Vascular tone researchCardiovascular ResearchModerate
- Pulmonary hypertension researchCardiovascular ResearchLow
- Endothelin system dissectionPharmacological ToolHigh
- Tumor vasculature modulationOncology ResearchLow
Contraindications
- Clinical therapeutic useRegulatoryHigh
- PregnancyPopulationHighPotential fetal risk or insufficient safety data
Adverse Effects
- Blood pressure elevationCardiovascularUnknown
- Injection site reactionsLocalUnknown
- VasoconstrictionCardiovascularUnknown
Drug Interactions
- BQ-123 (ET-A antagonist)Moderate
- Endothelin-1Low
Population Constraints
- General human population (therapeutic)Regulatory ConstraintAbsolute
- Pregnant subjectsReproductiveRelative
Regulatory Status
- European UnionUnapprovedNo EMA approval; used only in preclinical and academic research.
- United StatesUnapprovedResearch compound only; not FDA approved for any indication.
- United KingdomUnapprovedNo MHRA approval; research use only.
BQ-788 has no regulatory approval in any jurisdiction. It is used exclusively as a research compound in preclinical and some early clinical investigational studies.
Evidence & Sources
No sources recorded yet.