Endothelin

AP Davenport, KA Hyndman, N Dhaun, C Southan… - Pharmacological …, 2016 - ASPET
The endothelins comprise three structurally similar 21-amino acid peptides. Endothelin-1
and-2 activate two G-protein coupled receptors, ETA and ETB, with equal affinity, whereas …

Cardiovascular Drug Interactions With Nirmatrelvir/Ritonavir in Patients With COVID-19: JACC Review Topic of the Week

S Abraham, A Nohria, TG Neilan, A Asnani… - Journal of the American …, 2022 - jacc.org
Nirmatrelvir-ritonavir (NMVr) is used to treat symptomatic, nonhospitalized patients with
coronavirus disease-2019 (COVID-19) who are at high risk of progression to severe …

[HTML][HTML] Endothelin receptors and their antagonists

JJ Maguire, AP Davenport - Seminars in nephrology, 2015 - Elsevier
All three members of the endothelin (ET) family of peptides, ET-1, ET-2, and ET-3, are
expressed in the human kidney, with ET-1 being the predominant isoform. ET-1 and ET-2 …

Randomized dose-response study of the new dual endothelin receptor antagonist aprocitentan in hypertension

P Verweij, P Danaietash, B Flamion, J Ménard… - …, 2020 - Am Heart Assoc
This study examined the dose-response characteristics of aprocitentan, a dual endothelin
A/endothelin B receptor antagonist, in patients with essential hypertension. In a randomized …

Aprocitentan and the endothelin system in resistant hypertension

M Clozel - Canadian Journal of Physiology and Pharmacology, 2022 - cdnsciencepub.com
Endothelin has emerged as a target for therapeutic intervention in systemic hypertension. As
a vasoconstrictor, comitogenic agent, linking pulse pressure and vascular remodeling, and …

Endothelin-receptor antagonists in the management of pulmonary arterial hypertension: where do we stand?

M Correale, A Ferraretti, I Monaco… - Vascular health and …, 2018 - Taylor & Francis
Pulmonary arterial hypertension, a disease largely neglected until a few decades ago, is
presently the object of intense studies by several research teams. Despite considerable …

Clinical pharmacokinetics and pharmacodynamics of the endothelin receptor antagonist macitentan

PN Sidharta, A Treiber, J Dingemanse - Clinical pharmacokinetics, 2015 - Springer
Pulmonary arterial hypertension (PAH) is a progressive disease of the lung vascular system,
which leads to right-sided heart failure and ultimately death if untreated. Treatments to …

[HTML][HTML] New insights into phenotypic switching of VSMCs induced by hyperhomocysteinemia: Role of endothelin-1 signaling

Y Chen, X Su, Q Qin, Y Yu, M Jia, H Zhang, H Li… - Biomedicine & …, 2020 - Elsevier
Phenotypic switching of vascular smooth muscle cells (VSMCs) plays a key role in
atherosclerosis. Hyperhomocysteinemia (HHcy) is an independent risk factor for …

Treatment of pulmonary arterial hypertension with the dual endothelin receptor antagonist macitentan: clinical evidence and experience

C Belge, M Delcroix - Therapeutic Advances in Respiratory …, 2019 - journals.sagepub.com
Macitentan (10 mg once daily orally), a dual endothelin receptor antagonist (ERA)
developed by modifying the structure of bosentan to increase the efficacity and safety, is …

From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective

C Boss, MH Bolli, J Gatfield - Bioorganic & Medicinal Chemistry Letters, 2016 - Elsevier
The endothelin peptides bind to two receptors found on cells of vasculature and in tissues.
While the endothelin-A (ETA)-receptor is predominantly expressed in vascular smooth …