Formoterol hemifumarate
β2 adrenergic agonist / Potent, long-acting agonist specific to β2 (Ki = 7.6 nM), but not β1 (Ki > 2.6 µM), adrenergic receptors in trachea (pD2 = 9.3) over atrium (pD2 = 7.0).1,2 Reduces adhesion and superoxide anion production in cultured activated eosinophils.3 Reverses cachexia in rats and mice via inhibition of the ATP-ubiquitin-dependent proteolytic system.4 Rescues LPS-induced motor function deficits and nigrostriatal dopamine loss in a rat model of Parkinson’s.5 Clinically useful for respiratory diseases.
Biochemicals & reagents
43229-80-7
BD 40A
1) Anderson et al. (1993), Formoterol: pharmacology, molecular basis of agonism and mechanism of long duration of a highly potent and selective beta 2-adrenoceptor agonist bronchodilator; Life Sciences, 52 2145 2) Teng et al. (2005), Structure-activity relationship study of novel necroptosis inhibitors; Bioorg. Med. Chem. Lett., 15 5039 3) Noguchi et al. (2015), Effect of beta2-adrenergic agonist on eosinophil adhesion, superoxide anion generation, and degranulation; Allergol. Int., 64 S46 4)Busquets et al. (2004), Anticachectic effects of formoterol: a drug for potential treatment of muscle wasting; Cancer Res., 64 6725 5) O’Neill et al. (2020), Pharmacological targeting of ß2-adrenoceptors is neuroprotective in the LPS inflammatory rat model of Parkinson’s disease; Br. J. Pharmacol., 177 282
RT
TARGET: GPCR -- PATHWAY: Cation channel; Calcium signaling -- RESEARCH AREA: Immunology; Neuroscience; Ubiquitin/Proteasome -- DISEASE AREA: Inflammation; Neurodegeneration