Endothelin receptor antagonists Rationale and mechanism of action
Medical > Therapy > Specific treatments
Endothelin receptor antagonists
Rationale and mechanism of action
Endothelin (ET) is an endogenous peptide with potent vasoconstrictor, mitogenic, and profibrotic effects (Miyauchi et al. 1999), and appears to play an important role in the pathogenesis of PAH. These patients have increased plasma ET levels (Stewart et al. 1991) and increased expression of ET in the pulmonary vasculature (Giaid et al. 1993). Levels of ET may correlate with pulmonary hemodynamics and exercise capacity (Rubens et al. 2001). Two distinct ET receptor isoforms have been identified, ETA and ETb (Benigni et al. 1999). Activation of ETA receptors induces sustained vasoconstriction and proliferation of vascular smooth muscle cells. In contrast, ETB receptors are mainly involved in clearance of ET, particularly in the vascular beds of the lungs and the kidneys. In addition they may have some vasodilatory effects.
References
Back to > Medical > Therapy > Specific treatments
Endothelin receptor antagonists
Rationale and mechanism of action
Endothelin (ET) is an endogenous peptide with potent vasoconstrictor, mitogenic, and profibrotic effects (Miyauchi et al. 1999), and appears to play an important role in the pathogenesis of PAH. These patients have increased plasma ET levels (Stewart et al. 1991) and increased expression of ET in the pulmonary vasculature (Giaid et al. 1993). Levels of ET may correlate with pulmonary hemodynamics and exercise capacity (Rubens et al. 2001). Two distinct ET receptor isoforms have been identified, ETA and ETb (Benigni et al. 1999). Activation of ETA receptors induces sustained vasoconstriction and proliferation of vascular smooth muscle cells. In contrast, ETB receptors are mainly involved in clearance of ET, particularly in the vascular beds of the lungs and the kidneys. In addition they may have some vasodilatory effects.
References
Back to > Medical > Therapy > Specific treatments
Druckversion
Suche
SSPH Research Prize 2012
Deadline for submission: April 30, 2012
Further information
Symposium "pulmonal-arterielle Hypertension im Kindesalter"
Donnerstag, 10. Mai 2012, 16.00-18.00, Bern
Further information:
5th International Congress of the Swiss Society of Pulmonary Hypertension (SSPH)
28.-29. September 2012, Thun, Congress Hotel Seepark Thun
Informationen: www.imk.ch/sgph2012
mehr