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Target intelligence / Profile preview
Endothelin Receptor (ETR)
- Target
- ETR
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
Endothelin receptors are a family of G protein-coupled receptors that mediate the effects of endothelins, potent vasoactive peptides. The main subtypes, ETA and ETB, play critical roles in regulating vascular tone, cell proliferation, and sodium/water balance. Dysregulation of endothelin receptor signaling is implicated in various cardiovascular and other diseases, making them important therapeutic targets.
- Other names
- ETA receptorETB receptorET-A receptorET-B receptorETARETBREndothelin type A receptorEndothelin type B receptor
02
Mechanism of action
Selective antagonism of ETA or ETB receptors, leading to vasodilation and/or reduced cell proliferation.
03
Biological functions
VasoconstrictionVasodilationCell proliferationNitric oxide releaseSodium retentionSalt/water balance regulationNeurotransmission modulationAngiogenesis regulation
04
Disease associations
HypertensionAtherosclerosisHeart failurePulmonary hypertensionGlomerulosclerosisCancer progressionNeuropathies
05
Safety considerations
Potential for blood pressure dysregulationSide effects related to vasodilation (e.g., headache, flushing)
06
Interacting drugs
BQ123
2 more in the full profile.
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