(R,R)-Formoterol β2-selective adrenergic agonist

Description: IC50 Value: N/A Formoterol is a novel highly β2-selective adrenergic agonist and holds promise as a β2-agonist that could impart selective beneficial metabolic effects. in vitro: Formoterol restored Dex sensitivity by inhibiting phosphorylation of GR-Ser226 and JNK1[1]. Formoterol (FM), but not SM, partially inhibited H(2) O(2) -induced PI3Kδ-dependent (PKB) phosphorylation. H(2) O(2) decreased SM-induced cAMP production in U937 cells, but did not significantly affect the response to FM [3]. in vivo: Mice exposed to formoterol for 24 or 72 h exhibited increases in kidney and heart mtDNA copy number, peroxisome proliferator-activated receptor γ coactivator 1α, and multiple genes involved in the mitochondrial electron transport chain (F0 subunit 6 of transmembrane F-type ATP synthase, NADH dehydrogenase subunit 1, NADH dehydrogenase subunit 6, and NADH dehydrogenase [ubiquinone] 1β subcomplex subunit 8) [2]. Formoterol and ritodrine inhibited the amplitude and frequency of rat uterine contraction, with IC50 values of 3.8 x 10(-10) and 4.7 x 10(-7) M, respectively [4]. Clinical trial: N/A ..