John Gatfield

TL;DR: Macitentan, by its tissue-targeting properties and dual antagonism of ET receptors, protects against end-organ damage in diabetes and improves survival in pulmonary hypertensive rats, which makes it a new agent to treat cardiovascular disorders associated with chronic tissue ET system activation.

TL;DR: Pharmacokinetic investigation of 8bo in beagle dogs suggests that the compound is suitable for once daily dosing in humans, and structure-activity relationships of a novel class of S1P(1) receptor agonists based on the 2-imino-thiazolidin-4-one scaffold are reported.

TL;DR: Macitentan is a competitive ERA with significantly slower receptor dissociation kinetics than the currently approved ERAs, which could contribute to an enhanced pharmacological activity of macitentan in ET-1-dependent pathologies.

TL;DR: In this paper, physicochemical data of two series of drug analogues of bosentan and vercirnon are documented as part of a comparative study of tert-butyl, pentafluorosulfanyl, trifluoromethyl, bicyclo[1.1]pentanyl, and cyclopropyl-trifluorsulfyl substituents.

TL;DR: A selective OXR-1 antagonist, represented by a phenylglycine-amide substituted tetrahydropapaverine derivative (ACT-335827), is described that is orally available, penetrates the brain, and decreases fear, compulsive behaviors and autonomic stress reactions in rats.