[HTML][HTML] Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells

J Gatfield, C Mueller Grandjean, T Sasse, M Clozel… - 2012 - journals.plos.org
Two endothelin receptor antagonists (ERAs), bosentan and ambrisentan, are currently
approved for the treatment of pulmonary arterial hypertension (PAH), a devastating disease …

[HTML][HTML] Distinct ETA Receptor Binding Mode of Macitentan As Determined by Site Directed Mutagenesis

J Gatfield, C Mueller Grandjean, D Bur, MH Bolli… - PLoS …, 2014 - journals.plos.org
The competitive endothelin receptor antagonists (ERA) bosentan and ambrisentan, which
have long been approved for the treatment of pulmonary arterial hypertension, are …

059 Daridorexant: A dual, equipotent, and insurmountable antagonist of both orexin-1 and orexin-2 receptors

CM Grandjean, M Kiry, C Vaillant, O Nayler, J Gatfield - Sleep, 2021 - academic.oup.com
Introduction The orexin neuropeptide–receptor system is a central sleep and wake regulator
in the brain. The two orexin receptor subtypes, OX1R and OX2R, are expressed either …

Unique receptor dissociation kinetics of the novel endothelin receptor antagonist macitentan

J Gatfield, CM Grandjean, T Sasse, B Steiner, P Steiner… - 2012 - Eur Respiratory Soc
Association and dissociation rates of G protein-coupled receptor antagonists can influence
their in vivo pharmacological activity, such as duration of action, activity in situations of …

061 Sleep Hygiene as an Intervention to Lower Blood Pressure

M Vazquez, H Yang, R Dang, M Haack, J Mullington - Sleep, 2021 - search.proquest.com
Methods Fifty participants (59.8±1.5 years; 31 women) completed 3 overnight in-hospital
stays. The first stay (S1) was a baseline control; the second stay (S2) followed a 4-week wait-list …

060 Challenging the current assessment criteria for scoring central sleep apnea at altitude

J Bird, J Chan, A Rimke, A Kalker, G Chan, T Brutsaert… - Sleep, 2021 - search.proquest.com
Methods We assessed CSA using portable polysomnography (ApneaLink, ResMed) during
ascent to 5160m in the Nepal Himalaya over 10 days in 15 healthy participants. Files were …

Evaluation of tert‐Butyl Isosteres: Case Studies of Physicochemical and Pharmacokinetic Properties, Efficacies, and Activities

MV Westphal, BT Wolfstädter, JM Plancher… - …, 2015 - Wiley Online Library
… We thank Célia Mueller Grandjean (Actelion Pharmaceuticals Ltd.) for technical assistance
with measurement of the bosentan analogues. SpiroChem is acknowledged for the generous …

Evaluating the efficacy of the selective orexin 1 receptor antagonist nivasorexant in an animal model of binge‐eating disorder

MA Steiner, L Botticelli, G Bergamini… - … Journal of Eating …, 2024 - Wiley Online Library
… Chemistry team (Idorsia) for the synthesis of the compounds, Manon Kiry and Celia Mueller
Grandjean for measuring the Kbs in the Calcium mobilization and IP 1 accumulation assay. …

Preparation, antiepileptic activity, and cardiovascular safety of dihydropyrazoles as brain-penetrant T-type calcium channel blockers

L Remen, O Bezençon, L Simons… - Journal of Medicinal …, 2016 - ACS Publications
A series of dihydropyrazole derivatives was developed as potent, selective, and brain-penetrating
T-type calcium channel blockers. An optimized derivative, compound 6c, was …

[BOOK][B] Merritt Island and Cocoa Beach

AE Parrish, AC Field, GL Harrell - 2001 - books.google.com
The history of Central Brevard County is almost as long and complicated as the geographical
borders of the county itself. Stretching north and south for 77 miles, Brevard County is a …