The selexipag active metabolite ACT-333679 displays strong anti-contractile and anti- remodeling effects, but low β-arrestin recruitment and desensitization potential

Authors: Gatfield J., Menyhart K., Wanner D., Gnerre C., Monnier L., Morrison K., Hess P., Iglarz M., Clozel M. and Nayler O

DOI: https://doi.org/10.1124/jpet.116.239665, 2017

Published in: The Journal of Pharmacology and Experimental Therapeutics

Tags: Single cell characterization, drug discovery, mitochondria and cell metabolism, Prostacyclin, PGI2, receptor, pulmonary arterial hypertension, PAH, cAMP, vasoconstriction, PASMC, extracellular matrix, Selexipag, Uptravi, cell proliferation, agonism, iloprost, beraprost, treprostinil, b-arrestin, internalization, baised agonism, cardiovascular drugs, G protein coupled signaling, receptor desensitization