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Description: Batefenterol (formerly known as GSK961081 and TD-5959) is a novel, potent and selective muscarinic receptor antagonist and beta2-adrenoceptor agonist; it displays high affinity for hM2, hM3 muscarinic and hbeta2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively. In a phase 2b trial, batefenterol produced statistical and clinically significant differences compared to placebo and numerically greater improvements in the primary end point of trough FEV1 compared to salmeterol after 4 weeks of dosing in patients with moderate to severe chronic obstructive pulmonary disease (COPD).
References: J Pharmacol Exp Ther. 2014 Oct; 351(1):190-9.; J Med Chem. 2015 Mar 26; 58(6):2609-22.
Related CAS#: 945905-37-3(succinate) 743461-65-6 (free base)
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